CO2017008600A2 - Análogos de desacetoxitubulisina h, composiciones y método de producción de los mismos - Google Patents

Análogos de desacetoxitubulisina h, composiciones y método de producción de los mismos

Info

Publication number
CO2017008600A2
CO2017008600A2 CONC2017/0008600A CO2017008600A CO2017008600A2 CO 2017008600 A2 CO2017008600 A2 CO 2017008600A2 CO 2017008600 A CO2017008600 A CO 2017008600A CO 2017008600 A2 CO2017008600 A2 CO 2017008600A2
Authority
CO
Colombia
Prior art keywords
analogs
present
compositions
deacetoxytubulysin
production
Prior art date
Application number
CONC2017/0008600A
Other languages
English (en)
Inventor
C Kyriacos Nicolaou
Dionosios 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 CO2017008600A2 publication Critical patent/CO2017008600A2/es

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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

Abstract

En un aspecto, la presente invención proporciona análogos de tubulisina de la fórmula: en donde R1, R2, R3, R4, X1, X2, X3, y A1 son como se definen en la presente descripción. En otro aspecto, la presente invención proporciona, además, métodos para preparar los compuestos descritos en en la presente descripción. En otro aspecto, la presente invención proporciona, además, composiciones farmacéuticas y métodos de uso de los compuestos descritos en en la presente descripción.
CONC2017/0008600A 2015-02-25 2017-08-25 Análogos de desacetoxitubulisina h, composiciones y método de producción de los mismos CO2017008600A2 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562120613P 2015-02-25 2015-02-25
US201662275667P 2016-01-06 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
CO2017008600A2 true CO2017008600A2 (es) 2018-02-09

Family

ID=56789084

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2017/0008600A CO2017008600A2 (es) 2015-02-25 2017-08-25 Análogos de desacetoxitubulisina h, composiciones y método de producción de los mismos

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)

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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
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
CR20200054A (es) 2017-08-09 2020-03-21 Denali Therapeutics Inc Compuestos, composiciones y métodos
TWI820038B (zh) 2017-09-08 2023-11-01 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
MX2021007235A (es) 2018-12-21 2021-09-23 Regeneron Pharma Tubulisinas y conjugados de proteina-tubulisina.
CN113518618A (zh) 2019-02-13 2021-10-19 戴纳立制药公司 化合物、组合物及方法
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)
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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AU2003253048A1 (en) 2002-07-09 2004-01-23 Morphochem Aktiengellschaft Fur Kombinatorische Chemie Tubulysin conjugates
AU2003266233A1 (en) * 2002-07-09 2004-01-23 Morphochem Aktiengesellschaft Fur Kombinatorische Chemie 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
CA2723671C (en) * 2007-05-10 2018-06-19 R & D Biopharmaceuticals Gmbh Tubulysine derivatives
WO2009012958A2 (en) 2007-07-20 2009-01-29 Helmholtz-Zentrum für Infektionsforschung GmbH Tubulysin d analogues
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JP2017510661A (ja) 2014-04-11 2017-04-13 メディミューン，エルエルシー ツブリシン誘導体

Also Published As

Publication number Publication date
CR20170438A (es) 2018-01-30
EP3261443B1 (en) 2021-04-28
BR112017018305A2 (pt) 2018-04-17
PH12017501539A1 (en) 2018-02-05
CN107529754A (zh) 2018-01-02
EP3261443A1 (en) 2018-01-03
IL254089A0 (en) 2017-10-31
HK1248069A1 (zh) 2018-10-12
MX2017011024A (es) 2017-10-20
JP2018509404A (ja) 2018-04-05
US10808007B2 (en) 2020-10-20
WO2016138288A1 (en) 2016-09-01
EP3261443A4 (en) 2018-09-26
DOP2017000202A (es) 2017-09-29
PE20180355A1 (es) 2018-02-21
SG11201706820RA (en) 2017-09-28
AU2016222575A1 (en) 2017-09-07
US20180127463A1 (en) 2018-05-10
GT201700190A (es) 2018-11-26
EA201791896A1 (ru) 2018-02-28
CA2977589A1 (en) 2016-09-01
KR20170137725A (ko) 2017-12-13
CL2017002170A1 (es) 2018-06-08
ECSP17057131A (es) 2019-03-29

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