DERIVATIVES OF 1-(2-OXOACETYL)-PIPERIDINE- OR PYRROLIDINE-2-CARBOXYLIC ACIDS, PHARMACEUTICAL COMPOSITION, METHOD OF TREATMENT, METHOD OF SYNTHESIS Russian patent published in 2000 - IPC

Abstract RU 2158258 C2

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes the novel derivatives of 1-(2-oxoacetyl)-piperidine- or pyrrolidine-2-carboxylic acids of the general formula (I) where A is oxygen atom; B and D mean independently Ar, direct or branched (C1-C10)-alkyl, direct or branched (C2-C10)-alkenyl or (C2-C10)-alkynyl; Ar means direct or branched substituted (C1-C6)-alkyl, direct or branched (C2-C6)-alkenyl or (C2-C6)-alkynyl being in each case one of CH2-groups of indicated alkyls, alkenyls or alkynyls can be optionally substituted with oxygen atom or the group of the formula (ii) where Q means hydrogen atom or direct or branched (C1-C6)-alkyl; T means Ar or 5-7-membered cycloalkyl substituted with hydroxy-group at position 4 under condition that at least one of B and D is taken independently from the group including direct or branched (C2-C10)-alkynyl; Ar means direct or branched substituted (C2-C6)-alkynyl where Ar means phenyl, 2-thienyl, 2-, 3- or 4-pyridyl, benzimidazolyl, 3H-indolyl, purinyl, 7-aza-indolyl and Ar can contain optionally 1-3 substituents taken independently among the group including hydroxy-group, hydroxymethyl-group, direct or branched O-(C1-C4)-alkenyl, O-phenyl, O-benzyl, carboxy-group, direct or branched N,N-di-C1-C5-alkyl, carboxamide, N-benzylcarboxamide, morpholinecarbonyl, thiomorpholinecarbonyl, N-methyl- or N-benzylpiperazinocarbonyl or the group of the formula -O-(CH2)q-X where X means 2-, 3- or 4-pyridyl, pyrazinyl or 2- or 3-thienyl; q is a whole number 0-2 where L means U and M means oxygen atom; U means direct or branched (C1-C6)-alkyl or Y where Y can contain optionally 1-3 substituents taken independently among the group consisting of direct or branched O-(C1-C4)-alkyl, O-benzyl, O-phenyl, direct or branched O-(C2-C4)-alkenyl, 1,2-methylenedihydroxy-group or 3-phenyl-(E)-prop.- -2-enyl; n = 1 or 2; m is a whole number 0-3. Novel compounds of the formula (I) maintain, enhance or recover sensitivity of cells to therapeutic or prophylactic agents. Invention relates to also pharmaceutical composition containing these compounds. These compounds and pharmaceutical compositions can be used for treatment of cells showing resistance to effect of many drugs, prevention of development of resistance to many drugs and for therapy of cancer disease showing resistance to many drugs. Invention describes also method of treatment and method of synthesis of compounds of the formula (I). EFFECT: new compounds indicated above, improved method of synthesis and treatment, valuable medicinal properties. 13 cl, 2 tbl, 13 ex

Similar patents RU2158258C2

Title Year Author Number
DERIVATIVES OF AMINO ACID, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION AND METHOD OF SUPPRESSION OF MULTIDRUG RESISTANCE 1995
  • Robert E. Zelle
  • Mehtt'Ju V. Kharding
RU2165410C2
SULFONEAMIDE INHIBITORS OF HIV-ASPARTYLPROTEASE, PHARMACEUTICAL COMPOSITION, METHOD OF TREATMENT, METHOD OF INHIBITOR IDENTIFICATION 1993
  • Rodzher D.Tang
  • Mark A.Marko
  • Govinda Rao Bkhisetti
RU2135496C1
METHODS AND COMPOSITIONS FOR GROWTH STIMULATION OF NEURITIS 1996
  • Armistid Dehvid M.
RU2197240C2
DERIVATIVES OF 3-[2-(3-ACYLAMINO-2-OXO-2H-PYRIDIN-1-YL)-ACETYLAMINO]-4-OXO-PENTANE ACID AND THEIR APPLICATION AS CASPASE INHIBITORS 2005
  • Sharr'E Zhan-Dam'En
  • Negtel Ronal'D
  • Mortimor Majkl
  • Stadli Dzhon R.
RU2412936C2
PEPTIDE KETONES, PHARMACEUTICAL COMPOSITION AND METHOD OF INHIBITION OF INTERLEUKIN-1β PROTEASE ACTIVITY 1994
  • Roland I.Dolli
  • Todd L.Grejbill
  • Gehri Dzh.Spejr
  • Kehterin P.Prouti
  • Stejnli Dzh.Shmidt
RU2133251C1
2-[4-[2-(2-AMINO-4-OXO-4,6,7,8-TETRAHYDRO-3H-PYRIMIDO-[5,4-B]- -[1,4]-THIAZINE-6-YL)ETHYL]BENZOYL (OR THIENYLCARBONYL)-AMINO]- -PENTANEDIOIC ACID OR ITS LOWER ALKYL ESTER, A METHOD OF INHIBITION AND PROLIFERATION OF CELLS AND A METHOD OF INHIBITION OF AN ENZYME ACTIVITY 1994
  • Majkl D.Varni
  • Sindija L.Palmer
  • Uill'Jam Kh.Romines
RU2127275C1
INHIBITORS OF BACTERIAL GYRASE AND THEIR APPLYING 2001
  • Grijo Ann-Lor
  • Charifson Pol
  • Stamos Din
  • Lajo Jusheng
  • Badia Majkl
  • Trjudo Martehn
RU2262932C2
METHOD OF PRODUCING BIARYLUREA AND ANALOGUES THEREOF 2006
  • Ehnsell Grehkhem
  • Blit Todd A.
  • Dzhouns Ehndrju D.
  • Littler Bendzhamin
  • Luker Adam
  • Najs Filip L.
  • Snunian Dzhon R.
RU2431630C2
METHODS AND INTERMEDIATE PRODUCTS 2006
  • Tehnouri Dzheral'D Dzh.
  • Chen' Min'Chzhan
  • Koshrehn Dzhon Eh.
RU2446171C2
METHODS AND INTERMEDIATE COMPOUNDS 2010
  • Tehnouri Dzheral'D Dzh.
  • Chehn' Min'Chzhan
  • Koshrehn Dzhon Eh.
  • Luker Adam
  • Jurkauskas Valdas
RU2531588C2

RU 2 158 258 C2

Authors

Dehvid M. Armistid

Dzheffri O. Saunders

Dzhoshua S. Boger

Dates

2000-10-27Published

1993-09-27Filed