1-{N-[2-(DIETHYLAMINO)ETHYL]-N-[4-(4-TRIFLUOROMETHYLPHENYL)-BENZYL]AMINOCA RBONYLMETHYL}-2-(4-FLUOROBENZYL)THIO-5,6-TRIMETHYLENEPYRIMIDINE-4-ONE OR ITS PHARMACEUTICALLY ACCEPTABLE SALT, METHOD FOR PREPARING AND PHARMACEUTICAL COMPOSITION Russian patent published in 2004 - IPC

Abstract RU 2235722 C2

FIELD: organic chemistry, chemical technology, medicine, pharmacy.

SUBSTANCE: invention relates to new 1-{N-[2-(diethylamino)ethyl]-N-[4-(4-trifluoromethylphenyl)-benzyl]aminocarbonylmethyl}-2-(4-fluorobenzyl)thio-5,6-trimethylenepyrimidine-4-one of the formula (I):

or its pharmaceutically acceptable salt that elicit properties of inhibitor of enzyme Lp-PLA2 and can be used for treatment or prophylaxis of morbidity state associated with activity of indicated enzyme. Such disease can be atherosclerosis and also diabetes, hypertension, stenocardia, reprefusion, ischemia, rheumatoid arthritis, Alzheimer's disease, myocardium infarction, sepsis, acute and chronic inflammation and psoriasis. Compounds can be used, in particular, for preparing a medicinal agent used for primary and secondary prophylaxis of acute coronary attacks. Compound of the formula (I) is prepared by interaction of compound of the formula (II):

with compound of the formula (III):

under conditions of amide formation. Invention relates also to a pharmaceutical composition.

EFFECT: improved preparing method, valuable medicinal properties of compound.

20 cl, 1 sch, 8 ex

Similar patents RU2235722C2

Title Year Author Number
DERIVATIVES OF NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS, METHODS FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION BASED ON THEREOF AND METHODS FOR TREATMENT OF INFLAMMATORY DISEASES AND RESPIRATORY WAYS DISEASES 2001
  • Bodkin Majkl
  • Ehriksson Tomas
  • Khansen Peter
  • Khemmerling Martin
  • Khenriksson Krister
  • Klingstedt Tomas
  • Pettersson Lars
RU2265011C2
NOVEL SUBSTITUTED INDOLES 2003
  • Bonnert Rodzher
  • Braf Stiven
  • Kuk Toni
  • Dikinson Mark
  • Rehjsehl Raksehjna
  • Sehndzhehjni Khajtesh
  • Tig Sajmon
RU2288914C2
OBTAINING AND USING TRICYCLIC PYRIMIDINONE COMPOUND AND COMPOSITION THEREOF 2021
  • Gu, Chzhenkhua
  • Van, Duntsin
  • Khu, Yukhun
RU2820903C1
INDOLE DERIVATIVES, THEIR OPTICAL ISOMERS AND PHARMACEUTICALLY ACCEPTABLE SALTS 1991
  • Dzhon Judzhin Makor[Us]
  • Martin Dzhejms Vites[Gb]
RU2095360C1
SULFONAMIDE GROUPS-CONTAINING HETEROCYCLIC COMPOUND, INTERMEDIATE COMPOUND AND ANTI-ANGIOGENIC AGENT BASED ON THEREOF 2000
  • Khaneda Toru
  • Tsuruoka Akikhiko
  • Kamata Juniti
  • Okabe Tadasi
  • Takakhasi Kejko
  • Nara Kazumasa
  • Khamaoka Siniti
  • Ueda Norikhiro
  • Vakabajasi Tosiaki
  • Funakhasi Jasukhiro
  • Semba Taro
  • Khata Naoko
  • Jamamoto Judzi
  • Ozava Eiti
  • Tsukakhara Naoko
  • Ova Takasi
RU2239631C2
DERIVATIVES OF (AZETHIDINE-1-YLALKYL)-LACTAMES, PHARMACEUTICAL COMPOSITION BASED ON THEREOF AND METHOD OF TREATMENT OF HUMANS WHEN PATIENTS ARE TREATED BY PRODUCING ANTAGONISTIC EFFECT ON TACHYKININ ACTING IN HUMAN NK-, NK- AND NK-RECEPTORS OR IN THEIR COMBINATION 1995
  • Makenzi Aleksandr Roderik
  • Marchington Alan Patrik
  • Middlton Donal'D Stjuart
  • Midouz Sandra Dora
RU2150468C1
INHIBITORS OF METALLOPROTEINASES, THEIR USING AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF 2002
  • Ehriksson Anders
  • Lepiste Matti
  • Lundkvist Mikaehl'
  • Munk Af Rozenskel'D Magnus
  • Zlatojdskij Pavol
RU2288228C2
NEW PYRROLO[3,2-d]PYRIMIDIN-4-ONE DERIVATIVES AND USING THEM IN THERAPY 2005
  • Begevig Anders
  • Lo-Alfredsson Ivonne
  • Pivonka Donald
  • Tiden Anna-Karin
RU2577858C2
PYRAZINONE DERIVATIVES AND USE THEREOF IN TREATMENT OF LUNG DISEASES 2008
  • Braf Stiven
  • Ehvans Richard
  • Luker Timoti Dzh.
  • Raubo Piotr
RU2479580C2
C-4 CARBONATE-COMPRISING TAXANES 2000
  • Kehdou Dzhon F.
  • Mastalerz Khehrold
  • Ksue Kiufen Mehj
  • Khehnsel Stiven
  • Zoekler Mehri Idson
  • Rouz Vil'Jam S.
  • Tehrrant Dzhejms G.
RU2243223C2

RU 2 235 722 C2

Authors

Khikki Deirdre Mehri Bernadett

Ajfe Robert Dzhon

Lich Kolin Ehndrju

Pinto Ivan Leo

Smit Stefen Allan

Stehnvej Stiven Dzhejms

Dates

2004-09-10Published

2001-02-13Filed