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1. US20160075726 - Tamoxifen derivatives for treatment of neoplastic diseases, especially with high HER2 protein level

Office
United States of America
Application Number 14786710
Application Date 07.04.2014
Publication Number 20160075726
Publication Date 17.03.2016
Grant Number 09896466
Grant Date 20.02.2018
Publication Kind B2
IPC
C07F 9/54
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9Compounds containing elements of Groups 5 or 15 of the Periodic System
02Phosphorus compounds
28with one or more P-C bonds
54Quaternary phosphonium compounds
A61K 31/135
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
13Amines, e.g. amantadine
135having aromatic rings, e.g. methadone
CPC
C07F 9/5442
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9Compounds containing elements of Groups 5 or 15 of the Periodic System
02Phosphorus compounds
28with one or more P—C bonds
54Quaternary phosphonium compounds
5442Aromatic phosphonium compounds (P-C aromatic linkage)
C07F 9/5449
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9Compounds containing elements of Groups 5 or 15 of the Periodic System
02Phosphorus compounds
28with one or more P—C bonds
54Quaternary phosphonium compounds
5449Polyphosphonium compounds
C07F 9/5456
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9Compounds containing elements of Groups 5 or 15 of the Periodic System
02Phosphorus compounds
28with one or more P—C bonds
54Quaternary phosphonium compounds
5456Arylalkanephosphonium compounds
C09B 23/0008
CCHEMISTRY; METALLURGY
09DYES; PAINTS; POLISHES; NATURAL RESINS; ADHESIVES; COMPOSITIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
BORGANIC DYES OR CLOSELY-RELATED COMPOUNDS FOR PRODUCING DYES ; , e.g. PIGMENTS; MORDANTS; LAKES
23Methine or polymethine dyes, e.g. cyanine dyes
0008substituted on the polymethine chain
C09B 23/0025
CCHEMISTRY; METALLURGY
09DYES; PAINTS; POLISHES; NATURAL RESINS; ADHESIVES; COMPOSITIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
BORGANIC DYES OR CLOSELY-RELATED COMPOUNDS FOR PRODUCING DYES ; , e.g. PIGMENTS; MORDANTS; LAKES
23Methine or polymethine dyes, e.g. cyanine dyes
0008substituted on the polymethine chain
0025the substituent being bound through an oxygen atom
C09B 23/141
CCHEMISTRY; METALLURGY
09DYES; PAINTS; POLISHES; NATURAL RESINS; ADHESIVES; COMPOSITIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
BORGANIC DYES OR CLOSELY-RELATED COMPOUNDS FOR PRODUCING DYES ; , e.g. PIGMENTS; MORDANTS; LAKES
23Methine or polymethine dyes, e.g. cyanine dyes
14Styryl dyes
141Bis styryl dyes containing two radicals C6H5-CH=CH-
Applicants Smart Brain S.R.O.
Biotechnologicky Ustav Av Cr, V.V.I.
KKCG AG
Inventors Jiri Neuzil
Jan Stursa
Lukas Werner
Agents Fitzpatrick, Cella, Harper & Scinto
Title
(EN) Tamoxifen derivatives for treatment of neoplastic diseases, especially with high HER2 protein level
Abstract
(EN)

The subject of the invention are new mitochondrially targeted E/Z isomers of aliphatic triphenylphosphonium derivatives of tamoxifen where the aliphatic chain is alkyl or alkenyl, and their corresponding tertiary amine salts and/or their mixture (MitoTAX). Alkyl triphenylphosphonium derivatives of tamoxifen have the general formula (I), where n=8 to 12 and where Z is selected from the group of organic salts or inorganic salts. Alkenyl triphenylphosphonium derivatives of tamoxifen have the general formula IA, where n=6 to 10 and where Z has the above mentioned meaning. These compounds are applicable for the treatment of neoplastic disease, especially those with high HER2 protein levels. The drug for the treatment of neoplastic diseases according to the invention contains at least one E/Z isomer of aliphatic triphenylphosphonium derivatives of tamoxifen of the general formula (I) and/or IA or their corresponding salts of tertiary amine.


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