7-DEOXYDERIVATIVES OF TAXOL, DERIVATIVES OF BACCATINE, 10-PENTAFLUOROPHENYLBACCATINE, 7-[(METHYLTHIO)CARBONOTHIOYLHYD- -ROXY]-13-TRIETHYLSILYLHYDROXYBACCATINE, PHARMACEUTICAL COMPOSITION Russian patent published in 1998 - IPC

Abstract RU 2122545 C1

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention proposes 7-deoxyderivatives of taxol of the formula (I) where R1 means a group of the formula -C(O)Rz where Rz is a group of the formula RO or R and R means C1-C6--alkyl, phenyl; Rg is phenyl or 5-membered heteroaryl containing one atom of oxygen or sulfur; R2 means hydrogen atom or a group of the formula: -COOR where R means C1-C6-alkyl. Also, invention relates to derivatives of baccatine-III (II) that are intermediate compounds in synthesis of 7-deoxyderivatives of taxol of the formula (I) and particular intermediate compounds: 10-penta-fluorothioncarbonate-7-triethylsilylhydroxybaccatine-III of the formula (III), 7-[(methylthio)carbonothioylhydroxy]-10- -deacetylhydroxybaccatine-III of the formula (IV) and 7-[(methylthio)carbonothioylhydroxy] -13-triethylsilhydroxy-baccatine-III of the formula (V) using for synthesis of derivatives of baccatine-III of the formula (II). Also, invention proposes a pharmaceutical composition containing a compound of the formula (I) that shows antitumor activity and can be used for treatment of mammals with tumors. EFFECT: improved method of synthesis, enhanced effectiveness. 14 cl, 1 tbl, 42 ex

Similar patents RU2122545C1

Title Year Author Number
FLUOROTAXOLS, INTERMEDIATE COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHOD OF PATIENT TREATMENT 1993
  • Shu-Kh'Ju Chen
  • Vittorio Farina
  • Dolatraj Vias
  • Dzhojdip Kant
RU2131874C1
6,7-MODIFIED PACLITAXELS AND INTERMEDIATE COMPOUNDS 1993
  • Shu-Kh'Ju Chen
  • Vittorio Farina
  • Gregori Rot
  • Dzhon Kehdou
RU2125998C1
TAXANE DERIVATIVE PHOSPHONOOXYMETHYL ESTERS, INTERMEDIATE COMPOUNDS, ANTITUMOR PHARMACEUTICAL COMPOSITION, METHOD OF TUMOR GROWTH SUPPRESSION IN MAMMALS 1993
  • Erzhi Golik
  • Dolatraj Vias
  • Dzhon Dzh. Rajt
  • Genri Vong
  • Dzhon F.Kadou
  • Dzhon K.Totatil
  • Ven-Sen Li
  • Murrej A.Kaplan
  • Robert K.Perron
RU2136673C1
PACLITAXEL DERIVATIVES, PHARMACEUTICAL COMPOSITION AND METHOD OF TUMOR GROWTH INHIBITION 1996
  • Pol M. Skola
  • Dzhon F. Kehdou
  • Dolatraj M. Vias
RU2162082C2
SIDE CHAIN TAXANES, INTERMEDIATE COMPOUNDS, AND METHODS OR PREPARING, THEREOF 1993
  • Mikaehl A.Poss
  • Dehvid Dzh.Kusera
  • Dzherom L.Moniot
  • Dzhon K.Tottatil
  • Ivan D.Trifunovich
  • Shu-Kh'Ju Chen
  • Dzhanmej Vej
RU2125042C1
CIS-N-IMINOMETHYL-3,4-DISUBSTITUTED-β-LACTAMS AND METHODS OF PREPARING CIS-3,4-DISUBSTITUTED-β-LACTAMS, AND USE THEREOF 1994
  • Allan V.Rehj
  • Parashotam Vemishetti
  • Roberto Drogini
RU2132844C1
DERIVATIVES OF N-ACYL-2-ARYLCYCLOALKYLAMINE STIMULATING MELATONIN SYNTHESIS, PHARMACEUTICAL COMPOSITION, METHOD OF MELATONIN-STIMULATING BINDING 1996
  • Dehniel Dzh. Kivi
  • Majkl F. Parker
  • Ronal'D Dzh. Mehttson
  • Grehkham Dzhonson
RU2162076C2
3-SUBSTITUTED OXINDOLE DERIVATIVES AS MODULATORS OF POTASSIUM CHANNELS, PHARMACEUTICAL COMPOSITION, METHOD OF TREATMENT 1996
  • Pijasena Khevavasam
  • Nikolas A. Minvell
  • Valentin K. Gribkov
RU2165925C2
BIPHENYLISOXAZOLSULFONAMIDES 1995
  • Nejtsen M'Jurudzhsan
  • Dzhoel S. Berrish
RU2174979C2
RETINOID-LIKE COMPOUNDS, PHARMACEUTICAL COMPOSITION, METHOD OF TREATMENT 1996
  • Dzhon E. Stehrrehtt Ml.
  • Kuo-Long Ju.
  • Muzammil M. Mansuri
  • Dehvid R. Tortolani
  • Peter R. Rezhek
RU2163590C2

RU 2 122 545 C1

Authors

Vittorio Farina

Shu-Kh'Ju Chen

Dehvid R.Lehngli

Mark D.Uittman

Dzhojdip Kehnt

Dolatraj Vajs

Dates

1998-11-27Published

1993-07-30Filed