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1. WO1996003364 - BENZOYLETHYLENE DERIVATIVE

Publication Number WO/1996/003364
Publication Date 08.02.1996
International Application No. PCT/JP1995/001475
International Filing Date 25.07.1995
IPC
C07C 59/90 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
59Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O-metal, -CHO, keto, ether, groups, groups, or groups
40Unsaturated compounds
76containing keto groups
90containing singly bound oxygen-containing groups
C07C 69/738 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
69Esters of carboxylic acids; Esters of carbonic or haloformic acids
66Esters of carboxylic acids having esterified carboxyl groups bound to acyclic carbon atoms and having any of the groups OH, O-metal, -CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
73of unsaturated acids
738Esters of keto-carboxylic acids
C07C 225/16 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
225Compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly-bound oxygen atoms not being part of a -CHO group, e.g. amino ketones
02having amino groups bound to acyclic carbon atoms of the carbon skeleton
14the carbon skeleton being unsaturated
16and containing six-membered aromatic rings
C07C 225/20 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
225Compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly-bound oxygen atoms not being part of a -CHO group, e.g. amino ketones
20having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of the carbon skeleton
C07C 229/44 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
229Compounds containing amino and carboxyl groups bound to the same carbon skeleton
40having amino groups bound to carbon atoms of at least one six-membered aromatic ring and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
44with carboxyl groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by unsaturated carbon chains
C07C 235/78 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
235Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
70having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
72with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms
76of an unsaturated carbon skeleton
78the carbon skeleton containing rings
CPC
C07C 225/16
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
225Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones
02having amino groups bound to acyclic carbon atoms of the carbon skeleton
14the carbon skeleton being unsaturated
16and containing six-membered aromatic rings
C07C 225/20
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
225Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones
20having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of the carbon skeleton
C07C 229/44
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
229Compounds containing amino and carboxyl groups bound to the same carbon skeleton
40having amino groups bound to carbon atoms of at least one six-membered aromatic ring and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
44with carboxyl groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by unsaturated carbon chains
C07C 235/78
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
235Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
70having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
72with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms
76of an unsaturated carbon skeleton
78the carbon skeleton containing rings
C07C 255/40
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
255Carboxylic acid nitriles
01having cyano groups bound to acyclic carbon atoms
32having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring
40the carbon skeleton being further substituted by doubly-bound oxygen atoms
C07C 255/41
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
255Carboxylic acid nitriles
01having cyano groups bound to acyclic carbon atoms
32having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring
41the carbon skeleton being further substituted by carboxyl groups, other than cyano groups
Applicants
  • MITSUBISHI CHEMICAL CORPORATION [JP/JP]; 5-2, Marunouchi 2-chome Chiyoda-ku, Tokyo 100, JP (AllExceptUS)
  • KITANO, Yasunori [JP/JP]; JP (UsOnly)
  • INOKAWA, Haruki [JP/JP]; JP (UsOnly)
  • TAKAYANAGI, Hisao [JP/JP]; JP (UsOnly)
  • YANO, Tamaki [JP/JP]; JP (UsOnly)
  • UMEKI, Hiroe [JP/JP]; JP (UsOnly)
  • HARA, Hiroto [JP/JP]; JP (UsOnly)
Inventors
  • KITANO, Yasunori; JP
  • INOKAWA, Haruki; JP
  • TAKAYANAGI, Hisao; JP
  • YANO, Tamaki; JP
  • UMEKI, Hiroe; JP
  • HARA, Hiroto; JP
Agents
  • HASEGAWA, Koji; Mitsubishi Chemical Corporation 5-2, Marunouchi 2-chome Chiyoda-ku Tokyo 100, JP
Priority Data
6/17535727.07.1994JP
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) BENZOYLETHYLENE DERIVATIVE
(FR) DERIVE DU BENZOYLETHYLENE
Abstract
(EN)
A benzoylethylene derivative represented by general formula (I) and a salt thereof wherein R1 to R5 represent each hydrogen, -OR9 (R9 being hydrogen, C1-C5 alkyl, etc.), etc.; R6 represents hydrogen, C1-C5 alkyl, etc.; R7 represents hydrogen, cyano, C1-C5 alkyl, -SOqR15 (q being 0, 1 or 2, and R15 being thienyl, phenyl, etc.), etc.; and R8 represents cyano, -CR22R23X (R22 and R23 being each hydrogen, C1-C5 alkyl, etc., and X being -NR24R25 (wherein R24 and R25 represent each C1-C5 alkyl, or R24 and R25 are combined together to represent alkylene, etc.)), etc. The derivative has potent activities of tyrosine kinase inhibition and cancer cell growth inhibition and is useful as a carcinostatic agent.
(FR)
Dérivé du benzoyléthylène, et ses sels, de formule générale (1) dans laquelle R1 à R5 représentent chacun hydrogène, -OR9 (R9 représentant hydrogène, C1-C5 alkyle, etc.) etc.; R6 représente hydrogène, C1-C5 alkyle; R7 représente hydrogène, cyano, C1-C5 alkyle, -SOqR15 (q valant 0, 1, ou 2 et R15 équivalant à thyényle, phényle etc.), etc.; R8 représente, cyano, -CR22R23 (R22 et R23 représentant chacun hydrogène, C1-C5 alkyle etc., et X représentant -NR24R25 (R24 et R25 équivalant chacun à C1-C5 alkyle, ou R24 et R25 étant combinés ensemble pour représenter alkylène, etc.)), etc. Ce dérivé présente des activités puissantes d'inhibition de la tyrosine kinase et de la croissance des cellules cancéreuses, et s'avère utile comme agent cancérostatique.
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