Invention Grant
US08772272B2 Pyrido-and pyrimidopyrimidine derivatives as anti-proliferative agents
有权
吡啶并嘧啶并嘧啶衍生物作为抗增殖剂
- Patent Title: Pyrido-and pyrimidopyrimidine derivatives as anti-proliferative agents
- Patent Title (中): 吡啶并嘧啶并嘧啶衍生物作为抗增殖剂
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Application No.: US12724203Application Date: 2010-03-15
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Publication No.: US08772272B2Publication Date: 2014-07-08
- Inventor: Eddy Jean Edgard Freyne , Marc Willems , Pierre Henri Storck , Virginie Sophie Poncelet , Kristof Van Emelen , Peter Jacobus Johnnes Antonius Buijnsters , Werner Constant Johan Embrechts , Timothy Pietro Suren Perera
- Applicant: Eddy Jean Edgard Freyne , Marc Willems , Pierre Henri Storck , Virginie Sophie Poncelet , Kristof Van Emelen , Peter Jacobus Johnnes Antonius Buijnsters , Werner Constant Johan Embrechts , Timothy Pietro Suren Perera
- Applicant Address: BG Beerse
- Assignee: Janssen Pharmaceutica NV
- Current Assignee: Janssen Pharmaceutica NV
- Current Assignee Address: BG Beerse
- Priority: WOPCT/EP03/51058 20031218; WOPCT/EP03/51062 20031218
- Main IPC: A61K31/33
- IPC: A61K31/33 ; A61K31/519 ; C07D487/00 ; C07D487/18

Abstract:
The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein a1-a2=a3-a4 represents a divalent radical selected from N—CH═CH—CH, N—CH═N—CH or CH—CH═N—CH; Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR13—C1-5alkyl-, —C1-6alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O— or —NR11—; X2 represents —C1-2alkyl-, —O—C1-2alkyl, —O— or —O—CH2—; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen; R4 represents hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or R4 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R11 represents hydrogen; R12 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R13 represents Het14-C1-4alkyl, in particular morpholinyl-C1-4alkyl; Het2 represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferably methyl; Het14 represents morpholinyl; Het16 represents a heterocycle selected from morpholinyl or pyrrolidinyl; Ar4 represents phenyl; Ar5 represents phenyl optionally substituted with cyano.
Public/Granted literature
- US20100173913A1 PYRIDO-AND PYRIMIDOPYRIMIDINE DERIVATIVES AS ANTI-PROLIFERATIVE AGENTS Public/Granted day:2010-07-08
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