RU92004362A - TAXOL DERIVATIVES AND WATER-SOLUBLE TAXOL DERIVATIVES - Google Patents

TAXOL DERIVATIVES AND WATER-SOLUBLE TAXOL DERIVATIVES

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Publication number
RU92004362A
RU92004362A RU92004362/04A RU92004362A RU92004362A RU 92004362 A RU92004362 A RU 92004362A RU 92004362/04 A RU92004362/04 A RU 92004362/04A RU 92004362 A RU92004362 A RU 92004362A RU 92004362 A RU92004362 A RU 92004362A
Authority
RU
Russia
Prior art keywords
taxol
synthesized
taxol derivatives
water
oxy
Prior art date
Application number
RU92004362/04A
Other languages
Russian (ru)
Other versions
RU2043346C1 (en
Inventor
Дж.Ай Кингстон Дэвид
Зао Зи-Янг
Original Assignee
Вирджиния Тек Интеллекчуал Пропертиз, Инк.
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
Priority claimed from US07/573,731 external-priority patent/US5059699A/en
Application filed by Вирджиния Тек Интеллекчуал Пропертиз, Инк. filed Critical Вирджиния Тек Интеллекчуал Пропертиз, Инк.
Application granted granted Critical
Publication of RU2043346C1 publication Critical patent/RU2043346C1/en
Publication of RU92004362A publication Critical patent/RU92004362A/en

Links

Claims (1)

Синтезированы производные сульфированного 2'-акрилоилтаксола и сульфированного 2'-О-ацилкислого таксола, обладающие улучшенной растворимостью в воде и стабильностью с одновременным сохранением биоактивности. В частности, синтезирована натриевая соль 2'-[(3-сульфо-1-оксопропил)окси] таксола при взаимодействии таксола с акриловой кислотой и с последующей реакцией 2'-акрилоилтаксола с бисульфитом согласно реакции Михаэлиса. При взаимодействии 2'-сукцинилтаксола с солями тетрабутиламмония и таурина и 3-аминопропилсульфокислотой соответственно с последующим обменом аммония на натрий были синтезированы натриевые соли 2'-{[4-((2-сульфоэтил)амино)-1,4-диоксобутил] окси} таксола и 2'-{[4-((3-сульфопропил)амино)-1,4-диоксобутил]окси}таксола. При взаимодействии гликоля с 2-O-ацилкислым таксолом были синтезированы гликолевые производные 2'-O-ацилкислых таксолов, обладающие улучшенной растворимостью в воде.Derivatives of sulfonated 2'-acryloyltaxol and sulfonated 2'-O-acyl acid taxol have been synthesized, which have improved solubility in water and stability while maintaining bioactivity. In particular, the sodium salt of 2 '- [(3-sulfo-1-oxopropyl) oxy] taxol was synthesized by the interaction of taxol with acrylic acid and the subsequent reaction of 2'-acryloyltaxol with bisulfite according to the Michaelis reaction. In the interaction of 2'-succinyltaxol with salts of tetrabutylammonium and taurine and 3-aminopropylsulfonic acid, respectively, followed by the exchange of ammonium for sodium, sodium salts of 2 '- {[4 - ((2-sulfoethyl) amino) -1,4-dioxobutyl] oxy} were synthesized taxol and 2 '- {[4 - ((3-sulfopropyl) amino) -1,4-dioxobutyl] oxy} taxol. In the interaction of glycol with 2-O-acyl acid taxol, glycol derivatives of 2'-O-acyl acid taxols with improved water solubility were synthesized.
RU9292004362A 1990-08-28 1992-10-14 Derivatives of taxol and water soluble derivatives of taxol RU2043346C1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US573731 1990-08-28
US07/573,731 US5059699A (en) 1990-08-28 1990-08-28 Water soluble derivatives of taxol

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
RU5001413 Division

Publications (2)

Publication Number Publication Date
RU2043346C1 RU2043346C1 (en) 1995-09-10
RU92004362A true RU92004362A (en) 1996-12-20

Family

ID=24293168

Family Applications (2)

Application Number Title Priority Date Filing Date
SU915001413A RU2059630C1 (en) 1990-08-28 1991-08-27 Taxol acryloyl-derivatives and a method of their synthesis, water-soluble derivatives of taxol and a method of their synthesis (variants)
RU9292004362A RU2043346C1 (en) 1990-08-28 1992-10-14 Derivatives of taxol and water soluble derivatives of taxol

Family Applications Before (1)

Application Number Title Priority Date Filing Date
SU915001413A RU2059630C1 (en) 1990-08-28 1991-08-27 Taxol acryloyl-derivatives and a method of their synthesis, water-soluble derivatives of taxol and a method of their synthesis (variants)

Country Status (24)

Country Link
US (2) US5059699A (en)
EP (1) EP0473326A1 (en)
JP (1) JPH0699410B2 (en)
KR (1) KR0132157B1 (en)
CN (1) CN1059337A (en)
AU (2) AU645340B2 (en)
CA (1) CA2049160C (en)
CS (1) CS263291A3 (en)
EG (1) EG19914A (en)
FI (1) FI913651A7 (en)
HU (1) HU210326B (en)
IE (1) IE913015A1 (en)
IL (1) IL99183A0 (en)
MX (2) MX9100832A (en)
MY (1) MY107794A (en)
NO (1) NO913007L (en)
NZ (1) NZ239377A (en)
OA (1) OA10035A (en)
PL (4) PL166242B1 (en)
PT (1) PT98787A (en)
RU (2) RU2059630C1 (en)
TW (1) TW209214B (en)
YU (1) YU144891A (en)
ZA (1) ZA916450B (en)

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