2,4-DI(PHENYLAMINO)PYRIMIDINES, APPLIED IN TREATMENT OF NEOPLASTIC DISEASES, INFLAMMATORY DISORDERS AND IMMUNE SYSTEM DISORDERS Russian patent published in 2010 - IPC C07D239/48 C07D405/12 C07D403/12 C07D401/12 C07D401/14 A61K31/506 A61K35/00 A61P29/00 A61P37/00 

Abstract RU 2400477 C2

FIELD: medicine.

SUBSTANCE: invention relates to novel pyrimidine derivatives of formula (I) or their pharmaceutically acceptable salts which possess inhibiting activity with respect to focal adhesion kinase (FAK), proteintyrosinekinase ZAP-70, receptor of insulin-like growth factor 1 (IGF-1R), tyrosinekinase activity of anaplastic lymphoma (ALK) and fusion protein NPM-ALK. In formula (I) , R0, R1 and R2 independently represent hydrogen, C1-C8 alkyl, 5- or 6-member heterocycle, containing 1,2 or 3 heteroatoms, selected from N, O and S, C1-C8alkoxy group, C1-C8alkylsulphinyl, C1-C8alkylsulphonyl, C5-C10arylsulphonyl, halogen, carbamoyl, sulphamoyl, etc.; R3 represents C1-C8alkylsulphinyl, C1-C8alkylsulphonyl, C5-C10arylsulphonyl, carbamoyl or sulphamoyl; R4 represents hydrogen or C1-C8alkyl; R5 represents chlorine or bromine; R6 represents hydrogen; R7, R8, R9 and R10 independently represent C1-C8alkyl, C5-C10aryl, possibly substituted by 5- or 6-member heterocycle, containing 1, 2 or 3 heteroatoms, selected from N, O and S, where substituents are selected from C1-C8alkyl, hydroxy, hydroxy-C1-C8alkyl, C1-C8alkoxy C1-C8alkyl, cyano, oxo, C1-C8alkylamino, diC1-C8alkylamino, carbamoyl, C1-C8alkylcaronyl, 5-10-member heterocycle, containing 1, 2 or 3 heteroatoms, selected from N and O, which is probably substituted by C1-C8alkyl; C1-C8alkoxy group, halogen- C1-C8alkoxy group, etc; A represents C. Invention also relates to pharmaceutical composition and to application of compounds of formula (I) for preparation of medication.

EFFECT: novel compounds possess useful biologic activity.

15 cl, 61 ex

Similar patents RU2400477C2

Title Year Author Number
PYRIMIDINE DERIVATIVES 2003
  • Benteli Rol'F
  • Tsenke Gerkhard
  • Kuki Najdzhl Grehm
  • Dutaler Rudol'F
  • Toma Gebkhard
  • Fon-Matt Anette
  • Khonda Toshijuki
  • Matsuura Naoko
  • Nonomura Katsukhiko
  • Okhmori Osamu
  • Umemura Ichiro
  • Khinterding Klaus
  • Papageorgiou Kristos
RU2324684C2
NEW DERIVATIVES OF PHENYLPROPARGYL ESTER 2001
  • Lambert Klemens
  • Tseller Martin
  • Kunts Val'Ter
  • Sederbaum Fredrik
RU2259353C2
AGENTS FOR BINDING FILLER WITH ELASTOMER 2004
  • Fuso Franchesko
  • Zherste Mishel'
  • Knoblokh Gerrit
  • Rota-Graz'Ozi P'Er
RU2371456C2
PYRIMIDINE DERIVATIVES 2005
  • Kavakhara Ehjdzhi
  • Mijaki Takakhiro
  • Rezel' Iogannes
RU2395507C2
USING SMOOTHENED ANTAGONISTS FOR TREATING HEDGEHOG PATHWAY RELATED DISORDERS 2009
  • Marion Dorsh
  • Dzhon Eh. Monakhan
  • Majkl Patrik Morrissi
  • Shifehn Pan'
  • Dzhul'Et Uill'Jams
RU2519200C2
THIAZOLYL DIHYDROQUINAZOLINES 2007
  • Brandl' Triksi
  • Majer Udo
  • Khenke Kristof
  • Jergensen Anne T.
  • Pauch Aleksander
  • Brajtfel'Der Shteffen
  • Grauert Mattias
  • Khoffmann Mattias
  • Shojerer Shtefan
  • Ehrb Klaus
  • Piper Mikhaehl'
  • Pragst Ingo
RU2430923C2
PYRIMIDINE DERIVATIVES 2005
  • Imbakh Patritsija
  • Kavakhara Ehjdzhi
  • Konishi Kazukhide
  • Matsuura Naoko
  • Mijake Takakhiro
  • Okhmori Osamu
  • Resel' Iogannes
  • Teno Naoki
  • Umemura Ichiro
RU2401260C2
NOVEL TRICYCLIC DERIVATIVES (VARIANTS), PHARMACEUTICAL COMPOSITION (VARIANTS), METHOD FOR INHIBITION OF IMMUNE RESPONSE OR TREATMENT AND/OR PROPHYLAXIS OF ALLERGIC DISEASES (VARIANTS) 1999
  • Tanimoto Norikhiko
  • Khasegava Jasushi
  • Khaga Nobukhiro
RU2216533C2
SULFOXIDES OR SULFONES, GRAFTED POLYMERS (VARIANTS), POLYMERIC COMPOSITION, METHOD FOR GRAFTING AND METHOD FOR STABILIZING POLYMERS 2002
  • Majer Khans-Rudol'F
  • Knoblokh Gerrit
  • Rota-Graziozi P'Er
  • Ehvans Sam'Juehl
  • Dubs Paul'
  • Zherst'E Mishel'
RU2291874C2
PHENYL DERIVATIVES AS PPAR AGONISTS 2004
  • Akkermann Zhan
  • Ehbi Iogannes
  • Bindzheli Al'Fred
  • Greter Uve
  • Irt Zhorzh
  • Kun Bernd
  • Mehrki Khans-Peter
  • Mejer Markus
  • Mor Peter
  • Rajt Mat'Ju Blejk
RU2374230C2

RU 2 400 477 C2

Authors

Garsija-Ehcheverrija Karlos

Kanazava Takanori

Kavakhara Ehjdzhi

Masuja Kejichi

Matsuura Naoko

Mijake Takakhiro

Okhmori Osamu

Umemura Ichiro

Dates

2010-09-27Published

2004-03-12Filed