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1. WO2017004172 - TOTAL SYNTHESIS OF SHISHIJIMICIN A AND ANALOGS THEREOF

Publication Number WO/2017/004172
Publication Date 05.01.2017
International Application No. PCT/US2016/040047
International Filing Date 29.06.2016
IPC
A61K 31/192 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
19Carboxylic acids, e.g. valproic acid
192having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
CPC
A61K 31/706
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7042Compounds having saccharide radicals and heterocyclic rings
7052having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
706containing six-membered rings with nitrogen as a ring hetero atom
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 47/6803
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
68the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
A61K 47/6807
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
68the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
6807the drug or compound being a sugar, nucleoside, nucleotide, nucleic acid, e.g. RNA antisense
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07D 405/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
405Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
Applicants
  • WILLIAM MARSH RICE UNIVERSITY [US/US]; 6100 Main St. Houston, TX 77005, US
Inventors
  • NICOLAOU, Kyriacos, C.; US
  • LI, Ruofan; US
  • LU, Zhaoyong; US
  • SOHN, Te-Ik; US
  • WOODS, James; US
  • PITSINOS, Emmanouil, N.; US
Agents
  • LONG, S., Reid; US
Priority Data
62/186,19129.06.2015US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) TOTAL SYNTHESIS OF SHISHIJIMICIN A AND ANALOGS THEREOF
(FR) SYNTHÈSE TOTALE DE SHISHIJIMICINE A ET D'ANALOGUES DE CELLE-CI
Abstract
(EN)
In one aspect, the present disclosure provides shishijimicin analogs of the formula: wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, antibody drug conjugates of the compounds are also provided.
(FR)
La présente invention concerne, dans un de ses aspects, des analogues de shishijimicine présentant la formule suivante: dans laquelle les variables sont telles que définies dans la description. Selon un autre aspect, la présente invention concerne également des procédés de préparation desdits composés. Selon un autre aspect encore, la présente invention concerne des compositions pharmaceutiques et des méthodes d'utilisation desdits composés. En outre, la présente invention concerne des conjugués anticorps-médicament de ces composés.
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