PYRIMIDINE DERIVATIVES AS ALK-5 INHIBITORS Russian patent published in 2013 - IPC C07D401/14 C07D405/14 C07D413/14 A61K31/4427 A61K31/5377 A61K31/506 A61K31/435 A61P9/00 A61P11/00 A61P29/00 

Abstract RU 2485115 C2

FIELD: chemistry.

SUBSTANCE: invention relates to novel pyrimidine derivatives of formula (I) in free form or in form of a pharmaceutically acceptable salt or solvate, which are useful in treating inflammatory or obstructive airways, pulmonary hypertension, pulmonary fibrosis, liver fibrosis, muscle diseases and systemic skeletal disorders and other diseases which are mediated by activity of the ALK-5 receptor or ALK-4 receptor. The invention also relates to a method of producing compounds of formula (I) and pharmaceutical compositions. In formula , T is a pyridin-2-yl which is optionally substituted in one position with R1; T1 is a pyridinyl which is optionally substituted in one or two positions with R1, R2, R5, C1-C4-alkoxy group, C1-C4-alkoxycarbonyl or cyano group; and Ra and Rb are independently hydrogen; C1-C8-alkyl, optionally substituted in one, two or three positions with R4; C3-C10-cycloalkyl, which is optionally substituted in one or two positions with a hydroxy group, amino group, C1-C8-alkyl, C1-C8-alkoxy group, halogen, cyano group, oxo group, carboxy group or nitro group; or C6-C15-aryl, optionally substituted in one, two or three positions with a halogen, hydroxy group, amino group, cyano group, oxo group, carboxy group, nitro group or R5; R1 is C1-C8-alkyl; R2 is C6-C15-aryl, optionally substituted in one, two or three positions with a halogen, hydroxy group, R1, R5, C1-C8-alkylthio group, amino group, C1-C8-alkylamino group, etc. The rest of the values of the radicals are given in the claim.

EFFECT: high efficiency of using said compounds.

20 cl, 2 tbl

Similar patents RU2485115C2

Title Year Author Number
MODULATORS OF ADENOSINE RECEPTORS 2001
  • Borroni Ehdilio Mauritsio
  • Khuber-Trottmann Gerda
  • Kilpatrik Gejvin Dzhon
  • Norkross Rozhe David
RU2277911C2
COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEREOF AND METHOD FOR TREATMENT OF CYTOKINE-MEDIATED DISEASE 2000
  • Betageri Radzhashekhar
  • Brejtfelder Steffen
  • Sirillo Pier F.
  • Dzhilmor Tomas A.
  • Khikej Judzhin R.
  • Kirrejn Tomas M.
  • Moriak Monika
  • Moss Nil
  • Patel Usha R.
  • Praudfut Dzhon R.
  • Regan Dzhon R.
  • Sharma Radzhiv
  • San Sanksin
  • Svinamer Alan D.
  • Takakhashi Khidenori
RU2298008C2
CYTOKINE INHIBITORS 2004
  • Chirillo P'Er Franchesko
  • Gao Donkhun Ami
  • Goldberg Daniel R.
  • Khammach Abdel'Khakim
  • Khao Minkhun
  • Kami Viktor Mark
  • Moss Nil
  • Neterton Rassel
  • Tsjan' Kevin Chun'Gen
  • Ralf Mark Stiven
  • U Lifen
  • Sjuj Dzhaomin
  • Ongst Ronald A. Dzhr.
RU2394029C2
COMPOUNDS USEFUL AS ANTI-INFLAMMATORY AGENTS 2000
  • Betageri Radzhashekhar
  • Brejtfelder Steffen
  • Sirillo Pier F.
  • Dzhilmor Tomas A.
  • Khikej Judzhin R.
  • Kirrejn Tomas M.
  • Moriak Monika
  • Moss Nil
  • Patel Usha R.
  • Praudfut Dzhon R.
  • Regan Dzhon R.
  • Sharma Radzhiv
  • San Sanksin
  • Svinamer Alan D.
  • Takakhashi Khidenori
RU2242474C2
NEW COMPOUNDS 2007
  • Serrano-Vu Majkl Kh.
  • Kvak En-Sin
  • Lju Vehn'Min
RU2456273C2
COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS 2005
  • Rehn' Pinda
  • Van Sja
  • Chzhan Guobao
  • Din Tsjan
  • Ju Shuli
  • Chzhan Tson
  • Chopiuk Greg
  • Albo Pamela A.
  • Sim Taebo
  • Grej Natanaehl Shiander
RU2401265C2
1,3-DIARYL-SUBSTITUTED UREAS AS KINASE ACTIVITY MODULATORS 2006
  • Mitchell Skott A.
  • Danka Mikhaela Dajana
  • Blomgren Piter A.
  • Desajmon Robert V.
  • Pippin Duglas A. I.
  • Brittelli Dehvid R.
RU2402544C2
COMPOUNDS AND COMPOSITIONS AS PROTEIN TYROSINE KINASE INHIBITORS 2006
  • Chzhan Guobao
  • Rehn' Pinda
  • Van Sja
  • Grej Natanael Sh.
  • Sim Taehbo
RU2386630C2
NEW PHTHALAZINONE DERIVATIVES AS AURORA A KINASE INHIBITORS 2005
  • Bojd Ehduard
  • Brukfild Frederik
  • Zhorzh Gi
  • Goller Bernkhard
  • Khjunsh Zabine
  • Rjuger Petra
  • Rjut Mattias
  • Shajblikh Shtefan
  • Shjull' Kristine
  • Fon-Der-Zal Vol'Fgang
  • Uorn Dzhastin
  • Vajgand Shtefan
RU2397166C2
COMPOUNDS AND COMPOSITIONS AS PROTEINKINASE INHIBITORS 2005
  • Van' Juntsin'
  • Mi Juan'
  • Fan' I
  • Chehn Daj
  • Lju I
  • Grej Natanaehl Shiander
  • Olbo Pamela A.
RU2406725C2

RU 2 485 115 C2

Authors

Leblan Katerine

Pipe Mod Nadin P'Errette

Fehrkherst Robin Alek

Adkok Klehr

Pults Robert Aleksander

Sho Dankan

Shtifl' Nikolaus Iogannes

Dates

2013-06-20Published

2007-07-12Filed