EP0288794A2
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EP
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Controlling the growth of tumor tissue with chalcone derivatives
Assignee: Aventis Pharmaceuticals Inc
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Filing: 1988-04-07
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Granted: —
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Expires: 2008-04-07
Abstract
Abstract Certain chalcone derivatives are reported to inhibit the polymerization of tubulin to form microtubules and are found to be antimitotic agents which can be used to control the growth of tumor tissue and can be used an antigout agents.
Inventors
- 👤 Michael L. Edwards
- 👤 David M. Stemerick
- 👤 Sai P. Sunkara
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-31 12:39
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/12; A61K31/16; A61K31/165; A61K31/13; A61K31/135
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
66 words
1) Use of a chalcone derivative of formula wherein Ar is a 2,5-dimethoxyphenyl, 2,3,4-trimethoxyphenyl, or 3,4,5-trimethoxyphenyl group; R₁ is a hydrogen, (C₁-C₄)alkyl, chloro, or bromo group; and R₂ is a -N(R)₂ or -NH(O)R wherein R is a (C₁-C₄)alkyl group or a pharmaceutically acceptable salt thereof for preparing a medicament for inhibiting the polymerization of tubulin to form microtubes or for inhibiting the growth of tumor tissues.
Claim 2
Dependent Claim
66 words
1) Use of a chalcone derivative of formula wherein Ar is a 2,5-dimethoxyphenyl, 2,3,4-trimethoxyphenyl, or 3,4,5-trimethoxyphenyl group; R₁ is a hydrogen, (C₁-C₄)alkyl, chloro, or bromo group; and R₂ is a -N(R)₂ or -NH(O)R wherein R is a (C₁-C₄)alkyl group or a pharmaceutically acceptable salt thereof for preparing a medicament for inhibiting the polymerization of tubulin to form microtubes or for inhibiting the growth of tumor tissues.
Claim 3
Dependent Claim
19 words
2) Process according to claim 1 wherein R₁ in the chalcone derivative of formula I represents a (C₁-C₄)alkyl group.
Claim 4
Dependent Claim
19 words
3) Process according to claim 1 wherein R₁ in the chalcone derivative of formula I represents a methyl group.
Claim 5
Dependent Claim
27 words
4) Process according to claims 1, 2, 3 wherein R₂ in the chalcone derivative of formula I represents a group of formula N(R)₂ wherein R represents (C₁-C₄)alkyl.
Claim 6
Dependent Claim
19 words
5) Process according to claim 4 wherein R in the chalcone derivative of formula I represents a methyl group.
Claim 7
Dependent Claim
24 words
6) Process according to any one of claims 1 to 5 wherein Ar in the chalcone derivative of formula I represents a 2,5-dimethoxyphenyl group.
Claim 8
Dependent Claim
28 words
7) Process according to any one of claims 1 to 5 wherein R₁ is a methyl group, R₂ is a dimethylamino group, and Ar is a 2,5-dimethoxyphenyl group.
Claim 9
Dependent Claim
23 words
8) a pharmaceutical composition which comprises a compound of any one of claims 1 to 7 in admixture with a pharmaceutically acceptable carrier.
Claim 10
Dependent Claim
92 words
9) A process for preparing a compound of any one of claims 1 to 7 which comprises: a) reacting an acetophenone derivative of the formula: wherein R₃ is selected from the group consisting of hydrogen and (C₁-C₄)alkyl, and Ar is as defined as above, with a benzaldehyde derivative of the formula: wherein R₂ is as defined above, in the presence of a base catalyst; and b) when a compound of formula 1 is desired wherein R₁ is a chloro or bromo group, reacting the above obtained product with a suitable halogenating agent.
Claim 11
Dependent Claim
32 words
10) Use of a compound of any of claims 1 to 7 for preparing a medicament for controlling the growth of tumor tissues in conjunction or combination with a known antitumor agent.
Claim 12
Dependent Claim
26 words
11) A pharmaceutical composition for the use according to claim 10 wherein the dosage of the known antitumor agent is significantly lower than the usual one.
References Cited (Backward Citations)
No citation records indexed.
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