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Title:
モルホリニルキナゾリン
Document Type and Number:
Japanese Patent JP2013522249
Kind Code:
A
Abstract:
The invention relates to compounds of the formulae (I), (II) and (III) in which R1, R2, R3, R4, Y, W1, W2, L, A, Alk, Cyc, Ar, Het1, Het2, Hal and n have the meaning indicated in Claim 1, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitization of cancer cells to anticancer agents and/or ionizing radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumors, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I) by reaction of compounds of the formulae (II) and (III) and optionally conversion of a base or acid of the compounds of the formula (I) into one of their salts.

Inventors:
Medellsky, Werner
Fuchs, thomas
Zenke, frank
Application Number:
JP2012557426A
Publication Date:
June 13, 2013
Filing Date:
February 17, 2011
Export Citation:
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Assignee:
Merck Patent Gesellschaft mit beschraenkter Haftung
International Classes:
C07D239/94; A61K31/5377; A61K31/55; A61K45/00; A61P35/00; A61P35/02; A61P35/04; A61P43/00; C07D401/04; C07D401/14; C07D409/14; C07D413/14; C07D417/14
Domestic Patent References:
JP2010502665A2010-01-28
JPH0673025A1994-03-15
JP2009510043A2009-03-12
JP2007531752A2007-11-08
JP2005515201A2005-05-26
JP2013515743A2013-05-09
JP2000510115A2000-08-08
JP2009529557A2009-08-20
Foreign References:
WO2009020140A12009-02-12
WO2010014939A12010-02-04
WO2002020500A22002-03-14
WO2002066445A12002-08-29
WO2009013126A12009-01-29
WO2008118758A12008-10-02
Other References:
"RN:1189950-64-8,RN:1189902-41-7", REGISTRY(STN), JPN6014054493, 12 December 2014 (2014-12-12), ISSN: 0002973053
JOURNAL OF ORGANIC CHEMISTRY, vol. Vol.40(18), JPN6014054497, 1975, pages 2613 - 2621, ISSN: 0002973055
JOURANAL OF MEDICINAL CHEMISTRY, vol. Vol.46(25), JPN6014054499, 2003, pages 5445 - 5457, ISSN: 0002973056
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. Vol.21(2), JPN6014054500, 2011, pages 829 - 835, ISSN: 0002973057
JOURNAL OF HETEROCYCLIC CHEMISTRY, vol. Vol.3(1), JPN6014054495, 1966, pages 67 - 69, ISSN: 0002973054
Attorney, Agent or Firm:
Kiyoji Kuzuwa