DERIVATIVES OF N-(3-PIPERIDINYLCARBONYL)-BETA-ALANINE AS ANTAGONISTS OF PLATELET ACTIVATION FACTOR, METHOD OF SYNTHESIS, PHARMACEUTICAL COMPOSITION AND METHOD OF TREATMENT Russian patent published in 2000 - IPC

Abstract RU 2161155 C2

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes novel derivatives of N-(3-piperidinylcarbonyl)-beta-alanine of the general formula (I) where R1 means piperidinyl that can has amino-protective group; R2 means carboxy- or esterified carboxy-group; A1 means C1-C6-alkylene, C1-C6-alkanyl-idene; A2 means C1-C6-alkylene; A3 means C1-C6-alkylene that can has a single suitable substituent taken among the group including C1-C6-alkyl, C2-C6-alkenyl, C1-C6-alkynyl, cyano-, amino- -group, protected aminoacyl-group, C1-C6-alkylsulfonylamino- -C1-C6-alkyl, phenyl, phenyl-C1-C6-alkynyl, phenyl-C1-C6alkyl substituted with from 1 to 4 C1-C6-alkoxy-groups, halogen-C1-C6- alkyl, C1-C6-alkylenedioxy, C1-C6-alkyl substituted with unsaturated condensed 5-6-membered heterocyclic group containing from 1 to 4 nitrogen atoms, phenylsulfonyl-C1-C6- -alkyl and unsaturated 5-6-membered heterocyclic group containing from 1 to 4 nitrogen atoms; is the group where means piperidyl, tetrahydroquinolyl, pyrrolidinyl or morpholinyl; X means O or NH; Y means NH; Z means the group (a) where R3 is hydrogen atom or C1-C6-alkyl; l = 0 or 1; m = 0 or 1; n = 0 or 1, or its pharmaceutically acceptable salt. Novel compounds are antagonists of glyco-protein IIb/IIIa, inhibitors of platelet aggregation and inhibitors of binding fibrinogen with platelets. Invention describes also method of synthesis of proposed compounds, pharmaceutical preparation containing this compound and method of prophylaxis and/or treatment of patients or animals with diseases given in the description of invention. EFFECT: new compounds indicated above, improved method of synthesis, valuable medicinal properties. 32 cl, 1 tbl, 44 ex

Similar patents RU2161155C2

Title Year Author Number
POLYPEPTIDE COMPOUND, METHOD OF ITS SYNTHESIS AND PHARMACEUTICAL COMPOSITION 1995
  • Khidenori Oki
  • Masaki Tomisima
  • Akira Jamada
  • Khizasi Takazugi
RU2165423C2
AMIDINONAPHTYL DERIVATIVES AND PHARMACEUTICAL COMPOSITION 1995
  • Khirajama Fukusi
  • Kosio Khirojuki
  • Matsumoto Juzo
  • Kavasaki Tomikhisa
  • Kaku Sejdzi
  • Janagisava Isao
RU2154633C2
ETHANOLAMINE DERIVATIVES, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION, METHOD OF TREATMENT 1993
  • Juiti Siokava
  • Masanobu Nagano
  • Kijosi Taniguti
  • Kazukhiko Take
  • Takesi Kato
  • Kazunori Tsubaki
RU2125983C1
HETEROCYCLIC COMPOUNDS OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF AND INTERMEDIATE COMPOUNDS 1994
  • Taniguti Kiesi
  • Nagano Masanobu
  • Khattori Kojudzi
  • Tsubaki Kazunori
  • Okitsu Osamu
  • Tabuti Sejitiro
RU2176640C2
POLYPEPTIDE COMPOUNDS, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION, METHOD OF PROPHYLAXIS AND/OR THERAPEUTIC TREATMENT 1994
  • Khidenori Okhki
  • Masaki Tomisima
  • Akira Jamada
  • Khisasi Takasugi
RU2164230C2
METHOD OF SYNTHESIS OF PYRAZOLE DERIVATIVES OR THEIR PHARMACEUTICALLY ACCEPTABLE SALTS 1990
  • Matsuo Masaaki[Jp]
  • Tsudzi Kiesi[Jp]
  • Konisi Nobukie[Jp]
  • Nakamura Katsuja[Jp]
RU2021990C1
PYRAZOLE DERIVATIVES OR THEIR PHARMACEUTICALLY ACCEPTABLE SALTS 1993
  • Masaaki Matsuo
  • Kijosi Tsudzi
  • Takasi Ogino
  • Nobukijo Konisi
RU2128172C1
PEPTIDE DERIVATIVES OR THEIR PHARMACEUTICALLY ACCEPTABLE SALTS, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION, METHOD OF INHIBITION OF TACHYKININ EFFECT 1993
  • Masaaki Matsuo
  • Dajdzhiro Khagivara
  • Khirosi Mijake
RU2119922C1
GUANIDINE DERIVATIVES, METHOD OF PREPARATION THEREOF, AND METHOD FOR INHIBITING Na/H EXCHANGE IN CELLS 1994
  • Atsusi Kuno
  • Josikazu Inou
  • Khisasi Takasugi
  • Khiroaki Mizuno
  • Kumi Jamasaki
RU2141946C1
HETEROBICYCLIC DERIVATIVES, METHODS OF THEIR SYNTHESIS AND PHARMACEUTICAL COMPOSITION 1995
  • Norikhiko Simazaki
  • Sinja Vatanabe
  • Akikhiko Savada
  • Kejdzi Khemmi
RU2170737C2

RU 2 161 155 C2

Authors

Mitsuru Okhkubo

Fumie Takakhasi

Tosio Jamanaka

Khiroesi Sakai

Masajuki Kato

Dates

2000-12-27Published

1994-09-21Filed