Invention Grant
- Patent Title: 3-cyano-quinoline derivatives with antiproliferative activity
- Patent Title (中): 具有抗增殖活性的3-氰基 - 喹啉衍生物
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Application No.: US10596509Application Date: 2004-12-15
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Publication No.: US07655642B2Publication Date: 2010-02-02
- Inventor: Eddy Jean Edgard Freyne , Peter Jacobus Johannes Buijnsters , Kristof Van Emelen , Werner Constant Johan Embrechts , Timothy Pietro Suren Perera
- Applicant: Eddy Jean Edgard Freyne , Peter Jacobus Johannes Buijnsters , Kristof Van Emelen , Werner Constant Johan Embrechts , Timothy Pietro Suren Perera
- Applicant Address: BE Beerse
- Assignee: Janssen Pharmaceutica N.V.
- Current Assignee: Janssen Pharmaceutica N.V.
- Current Assignee Address: BE Beerse
- Priority: EPPCT/EP03/51059 20031218
- International Application: PCT/EP2004/053497 WO 20041215
- International Announcement: WO2005/058318 WO 20050630
- Main IPC: A01N43/00
- IPC: A01N43/00 ; A61K31/33 ; C07D487/00

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 Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR12—C1-5alkyl-, —C1-6alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O—; X2 represents a direct bond, —NR11—C1-2alkyl-, —NR11—CH2—, —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, hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or R3 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R10 represents hydrogen; R11 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R12 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
- US20080139601A1 3-Cyano-Quinoline Derivatives With Antiproliferative Activity Public/Granted day:2008-06-12
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