NOVEL DERIVATIVES OF ACETAMIDE, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION AND PROTEASE INHIBITORS BASED ON THEREOF Russian patent published in 2002 - IPC

Abstract RU 2181360 C2

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to novel compounds of the formula (I) where R0 means phenyl; R1 means phenyl, heteroaryl, lower alkyl that can be free or substituted; R2 means free or substituted phenyl, lower alkyl; R3 means hydrogen atom, acyl-group, sulfonyl-group; X and Y mean independently nitrogen or carbon atom; Z is methylene group. These compounds show inhibitory activity with respect to proteases of chymotrypsin type and can be used as inhibitors of indicated enzymes, especially as inhibitors of chymase and as an active component in pharmaceutical composition. Invention relates to a novel method of synthesis of derivatives of acetamide of the formula (I) by oxidation of compound of the formula (II) after removal of protective group of indicated compound if it presents. EFFECT: new compounds indicated above, improved method of their synthesis, valuable biochemical properties. 24 cl, 17 tbl

Similar patents RU2181360C2

Title Year Author Number
DERIVATIVES OF PHENANTHRIDINIUM SHOWING ANTITUMOR ACTIVITY, METHOD OF INHIBITION OF CANCER CELLS GROWTH 1997
  • Masuda Akira
  • Suva Masato
  • Suzuki Masanobu
RU2183626C2
METHOD OF PREPARING OPTICALLY ACTIVE ESTERS OF ERYTHRO-3-AMINO-2- HYDROXYBUTYRIC ACIDS AND CORRESPONDING ACIDS 1997
  • Satoo Khisao
  • Jamamoto Keniti
RU2169138C2
3-PHENYLCINNOLIN ANALOGUE AND BASED ON IT ANTI-TUMOR AGENT 2003
  • Kuroiva Sunsuke
  • Odanaka Dzunko
  • Marujama Sakiko
  • Sato Jositaka
  • Tomura Arikhiro
  • Sato Khirosi
  • Suzuki Josikazu
RU2324683C2
METHOD FOR IDENTIFICATION OF ANTI-TUMOR TARGET ENZYMES 2002
  • Isitsuka Khideo
  • Okabe Khisafumi
  • Simma Nobuo
  • Tsukuda Takuo
  • Umeda Isao
RU2319482C2
22-THIAVITAMIN D DERIVATIVES, METHOD OF PREPARATION THEREOF, METHOD FOR PREPARATION OF COMPOUNDS, AND COMPOUNDS 1995
  • Noboru Kubodera
  • Akira Kavase
RU2142941C1
[1,2,4]TRIAZOLO[1,5-a]PYRIMIDINE-2-YLUREA DERIVATIVE AND ITS APPLICATION 2004
  • Masuda Akira
  • Satokh Esitaka
  • Akijama Judzi
  • Sajga Kan
  • Tojoda Ehriko
RU2348636C2
QUINOLINE AND QUINAZOLINE DERIVATIVES 2000
  • Kubo Kazuo
  • Fudzivara Jasunari
  • Isoe Tosijuki
RU2256654C2
SYNTHESIS OF CARBAMOIL-PYRIDONE INHIBITORS OF HIV INTEGRASE AND INTERMEDIATE COMPOUNDS 2013
  • Joshida Khiroshi
  • Taoda Joshiyuki
  • Dzhons Brajan Alvin
  • Kavasuzhi Takashi
  • Nagamatsu Daiki
RU2638923C2
DERIVATIVES OF 2-THIOURACIL WITH ANTIADENOVIRAL ACTIVITY 2017
  • Novikov Mikhail Stanislavovich
  • Nikitenko Natalya Anatolevna
  • Ozerov Aleksandr Aleksandrovich
  • Gejsman Aleksandr Nikolaevich
  • Lysenko Kseniya Nikolaevna
  • Tukhvatulin Amir Ildarovich
  • Logunov Denis Yurevich
RU2670204C1
HYDRAZINE DERIVATIVE, INSECTICIDAL COMPOSITION, METHOD OF CONTROLLING PESTS, PROCESS FOR PREPARING HYDRAZINE DERIVATIVE 1992
  • Mikio Janagi[Jp]
  • Khirojasu Sugizaki[Jp]
  • Tetsuja Toja[Jp]
  • Jasukhito Kato[Jp]
  • Khidetosi Sirakura[Jp]
  • Tetsuo Vatanabe[Jp]
  • Esimi Jadzima[Jp]
  • Seiitirou Kodama[Jp]
  • Akio Masui[Jp]
  • Tosiaki Janai[Jp]
  • Esikhisa Tsukamoto[Jp]
  • Esikhiro Savada[Jp]
  • Sindzi Ekoi[Jp]
RU2041220C1

RU 2 181 360 C2

Authors

Sudzuki Esikadzu

Isida Koiti

Dates

2002-04-20Published

1997-09-05Filed