DOP2017000202A - Desacetoxitubulisina h y análogos de esta - Google Patents

Desacetoxitubulisina h y análogos de esta

Info

Publication number
DOP2017000202A
DOP2017000202A DO2017000202A DO2017000202A DOP2017000202A DO P2017000202 A DOP2017000202 A DO P2017000202A DO 2017000202 A DO2017000202 A DO 2017000202A DO 2017000202 A DO2017000202 A DO 2017000202A DO P2017000202 A DOP2017000202 A DO P2017000202A
Authority
DO
Dominican Republic
Prior art keywords
present
analogs
deacetoxitubulisine
present description
compounds described
Prior art date
Application number
DO2017000202A
Other languages
English (en)
Spanish (es)
Inventor
Yin Jun
Erande Rohan
Mandal Debashis
Klahn Philipp
C Nicolaou Kyriacos
Vourloumis Dionosios
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 DOP2017000202A publication Critical patent/DOP2017000202A/es

Links

Classifications

    • 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)
DO2017000202A 2015-02-25 2017-08-25 Desacetoxitubulisina h y análogos de esta DOP2017000202A (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
DOP2017000202A true DOP2017000202A (es) 2017-09-29

Family

ID=56789084

Family Applications (1)

Application Number Title Priority Date Filing Date
DO2017000202A DOP2017000202A (es) 2015-02-25 2017-08-25 Desacetoxitubulisina h y análogos de esta

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 (14)

* 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
WO2019008506A1 (en) * 2017-07-03 2019-01-10 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 THE TREATMENT OF CANCER AND OTHER DISEASES
IL301709B2 (en) 2017-08-09 2025-07-01 Denali Therapeutics Inc Compounds, compositions and methods
TW201920129A (zh) 2017-09-01 2019-06-01 美商戴納立製藥公司 化合物、組合物及方法
MA50124A (fr) * 2017-09-08 2020-07-15 Seattle Genetics Inc Procédé de préparation de tubulysines et d'intermédiaires de celles-ci
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
WO2020132658A2 (en) 2018-12-21 2020-06-25 Regeneron Pharmaceuticals, Inc. Tubulysins and protein-tubulysin conjugates
EP3924341A4 (en) 2019-02-13 2022-11-02 Denali Therapeutics Inc. Compounds, compositions and methods
CR20210426A (es) 2019-02-13 2021-09-30 Denali Therapeutics Inc Compuestos, composiciones y métodos
WO2021004516A1 (en) * 2019-07-11 2021-01-14 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)
TW202241857A (zh) 2020-12-18 2022-11-01 美商戴納立製藥公司 化合物之固體形式
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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1521769B1 (de) 2002-07-09 2015-09-09 Dömling, Alexander Tubulysinkonjugate
US7816377B2 (en) 2002-07-09 2010-10-19 R&D-Biopharmaceuticals Gmbh 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
EP2148886B1 (en) 2007-05-10 2014-02-19 R & D Biopharmaceuticals Gmbh Tubulysine derivatives
EP2181101A2 (en) 2007-07-20 2010-05-05 Helmholtz-Zentrum für Infektionsforschung GmbH Tubulysin d analogues
EP2209374B1 (en) * 2007-10-25 2014-12-03 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
US8889880B2 (en) * 2010-08-06 2014-11-18 Endocyte, Inc. Processes for preparing tubulysins
US20140080175A1 (en) 2012-03-29 2014-03-20 Endocyte, Inc. Processes for preparing tubulysin derivatives and conjugates thereof
DK2956173T3 (en) 2013-02-14 2017-07-17 Bristol Myers Squibb Co TUBULYSIS RELATIONSHIPS, METHODS OF PRODUCING AND USING THEREOF
CA2945318A1 (en) * 2014-04-11 2015-10-15 Medimmune, Llc Tubulysin derivatives

Also Published As

Publication number Publication date
WO2016138288A1 (en) 2016-09-01
GT201700190A (es) 2018-11-26
CL2017002170A1 (es) 2018-06-08
JP2018509404A (ja) 2018-04-05
CR20170438A (es) 2018-01-30
EP3261443A1 (en) 2018-01-03
IL254089A0 (en) 2017-10-31
EP3261443A4 (en) 2018-09-26
US20180127463A1 (en) 2018-05-10
AU2016222575A1 (en) 2017-09-07
US10808007B2 (en) 2020-10-20
CA2977589A1 (en) 2016-09-01
PE20180355A1 (es) 2018-02-21
BR112017018305A2 (pt) 2018-04-17
CO2017008600A2 (es) 2018-02-09
PH12017501539A1 (en) 2018-02-05
CN107529754A (zh) 2018-01-02
SG11201706820RA (en) 2017-09-28
KR20170137725A (ko) 2017-12-13
EP3261443B1 (en) 2021-04-28
MX2017011024A (es) 2017-10-20
EA201791896A1 (ru) 2018-02-28
ECSP17057131A (es) 2019-03-29
HK1248069A1 (zh) 2018-10-12

Similar Documents

Publication Publication Date Title
CR20170438A (es) Desacetoxitubulisina h y análogos de esta
CL2020003007A1 (es) Lactamas biciclicas y metodos de uso de las mismas (divisional solicitud no. 3486-2017)
NI201800128A (es) Derivados de carbonucleósidos sustituidos útiles como agentes antineoplásicos
GT201700189A (es) Derivados de nucleósidos sustituidos útiles como agentes antineoplásicos
CL2018003473A1 (es) Nuevos derivados piperidinilo sustituidos con hetero(arilo), un proceso para su preparación y composiciones farmacéuticas que los contienen.
CL2018003474A1 (es) Nuevos derivados piperidinilo, un proceso para su preparación y composiciones farmacéuticas que los contienen.
ECSP18053634A (es) Nuevos derivados de amonio, un proceso para su preparación y composiciones farmacéuticas que los contienen
UY36733A (es) Nuevos derivados aminoácido, un proceso para su preparación y composiciones farmacéuticas que los contienen
CR20160241A (es) Nuevas dihidroquinolizinonas para el tratamiento y profilaxis de la infección por virus de la hepatitis b
SV2017005587A (es) Nuevos derivados hidroxiester, un proceso para su preparacion y composiciones farmaceutacas que los contienen
MX373247B (es) Nuevos derivados de octahidro-pirrolo[3,4-c]-pirrol y análogos del mismo como inhibidores de atotaxina.
SV2017005590A (es) Nuevos derivados hidroxiacido un proceso para su preparacion y composiciones farmaceuticas que los contienen
CR20170575A (es) Nuevos derivados bicíclicos, un proceso para su preparación y composiciones farmacéuticas que los continen.
MX2018000511A (es) Derivados de fenoximetilo.
CO7210068A1 (es) Nuevos derivados tienopirimidina, un proceso para su preparación y composiciones farmacéuticas que los contienen
ECSP17069696A (es) Compuestos novedosos
CR20170484A (es) Azabenzimidazoles y su uso como moduladores del receptor ampa
UY38009A (es) Proceso para la preparación de derivados de quinolina
UY34612A (es) ?procedimiento para la preparación de derivados de isoxazolina azetidina quirales como agentes antiparasitarios?.
CR20140051A (es) Compuestos de tiazol y oxazol de bencen-sulfonamida
ECSP17046657A (es) Síntesis total de trioxacarcina dc-45-a2 y preparación de análogos de trioxacarcina
ECSP17063489A (es) Derivados de nucleósidos sustituidos útiles como agentes antineoplásicos
SV2014004879A (es) Nuevos derivados tienopirimidina, un proceso para su preparación y composiciones farmacéuticas que los contienen
UY35999A (es) Indol- y bencimidazolcarboxamidas como insecticidas y acaricidas