EP0192235A1
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Benzoyl urea compounds, process for their production, and antitumorous compositions containing them
Assignee: Ishihara Sangyo Kaisha Ltd
•
Filing: 1986-02-18
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Granted: —
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Expires: 2006-02-18
Abstract
Abstract A benzoyl urea compound having the formula:wherein A is a bromine atom or a chlorine atom.
Inventors
- 👤 Takahiro Haga
- 👤 Nobutoshi Yamada
- 👤 Hideo Sugi
- 👤 Toru Koyanagi
- 👤 Nobuo Kondo
- 👤 Tsunetaka Nakajima
- 👤 Masahiro Watanabe
- 👤 Kazumasa Yokoyama
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-01 13:27
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/02; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/44; A61K31/495; A61K31/505; A61K47/00; A61K47/06; A61K47/08; A61K47/10; A61K47/30; A61K47/36; A61K47/40; A61K47/44; A61K9/0012; A61K9/0019; A61K9/20; A61K9/2004; A61K9/2013; A61K9/48; A61K9/4841; A61K9/4858; C; C07; C07D; C07D239/00; C07D239/02; C07D239/24; C07D239/28; C07D239/32; C07D239/34
Claims Analysis
Total Claims: 36
Claim 1
Independent Claim
17 words
A benzoyl urea compound having the formula: wherein A is a bromine atom or a chlorine atom.
Claim 2
Dependent Claim
17 words
A benzoyl urea compound having the formula: wherein A is a bromine atom or a chlorine atom.
Claim 3
Dependent Claim
11 words
The benzoyl urea compound according to Claim 1, which is N-(2-nitrobenzoyl)-N'-[4-(3-bromo-2-pyrimidinyloxy)-3-chlorophenyl]urea.
Claim 4
Dependent Claim
11 words
The benzoyl urea compound according to Claim 1, which is N-(2-nitrobenzoyl)-N'-[3-chloro-4-(5-chloro-2-pyrimidinyloxy)phenyl]urea.
Claim 5
Dependent Claim
122 words
A process for producing a benzoyl urea compound having the formula: wherein A is a bromine atom or a chlorine atom, which comprises reacting a substituted nitrobenzene compound having the formula: wherein R1 is an isocyanate group, an amino group or a -NHCONH--OH group, with a substituted pyrimidine compound having the formula: wherein A is as defined above and R 2 is a halogen atom, or a R 3 . group wherein R 3 is an isocyanate group or an amino group which differs from R 1 with the proviso that when R 1 is an isocyanate group or an amino group, then R 2 is a group, and when R 1 is a then R 2 is a halogen atom. group,
Claim 6
Dependent Claim
122 words
A process for producing a benzoyl urea compound having the formula: wherein A is a bromine atom or a chlorine atom, which comprises reacting a substituted nitrobenzene compound having the formula: wherein R1 is an isocyanate group, an amino group or a -NHCONH--OH group, with a substituted pyrimidine compound having the formula: wherein A is as defined above and R 2 is a halogen atom, or a R 3 . group wherein R 3 is an isocyanate group or an amino group which differs from R 1 with the proviso that when R 1 is an isocyanate group or an amino group, then R 2 is a group, and when R 1 is a then R 2 is a halogen atom. group,
Claim 7
Dependent Claim
67 words
The process according to Claim 4, wherein the substituted nitrobenzene compound is a 2-nitrobenzoyl compound having the formula: wherein R' 1 is an isocyanate group or an amino group, and the substituted pyrimidine compound is a pyrimidinyloxybenzene compound having the formula: wherein A is a bromine atom or a chlorine atom, R 3 is an amino group or an isocyanate group which differs from R' 1 .
Claim 8
Dependent Claim
20 words
The process according to Claim 5, wherein R' 1 is an isocyanate group and R 3 is an amino group.
Claim 9
Dependent Claim
17 words
The process according to Claim 6, wherein the reaction is conducted in the presence of a solvent.
Claim 10
Dependent Claim
19 words
The process according to Claim 6, wherein the reaction is conducted at a temperature of from 0 to 120°C.
Claim 11
Dependent Claim
20 words
The process according to Claim 5, wherein R' 1 is an amino group and R 3 is an isocyanate group,
Claim 12
Dependent Claim
17 words
The process according to Claim 9, wherein the reaction is conducted in the presence of a solvent.
Claim 13
Dependent Claim
22 words
ll. The process according to Claim 9, wherein the reaction is conducted at a temperature of from 50°C to the refluxing temperature.
Claim 14
Dependent Claim
37 words
The process according to Claim 4, wherein the substituted nitrobenzene compound is N-(2-nitrobenzoyl)-N'-(3-chloro-4-hydroxyphenyl)urea, and the substituted pyrimidine compound has the formula: wherein A is a bromine atom or a chlorine atom, and Hal is a halogen atom.
Claim 15
Dependent Claim
21 words
The process according to Claim 12, wherein the reaction is conducted in the presence of an alkaline substance and a solvent.
Claim 16
Dependent Claim
21 words
The process according to Claim 12, wherein the reaction is conducted at a temperature of from 0°C to the refluxing temperature.
Claim 17
Dependent Claim
21 words
An antitumorous composition containing a benzoyl urea compound having the formula: wherein A is a bromine atom or a chlorine atom.
Claim 18
Dependent Claim
21 words
An antitumorous composition containing a benzoyl urea compound having the formula: wherein A is a bromine atom or a chlorine atom.
Claim 19
Dependent Claim
22 words
The antitumorous composition according to Claim 15, which comprises the benzoyl urea compound of the formula I and a pharmaceutically acceptable adjuvant.
Claim 20
Dependent Claim
15 words
The antitumorous composition according to Claim 16, wherein the pharmaceutically acceptable adjuvant is a surfactant.
Claim 21
Dependent Claim
18 words
The antitumorous composition according to Claim 16, wherein the pharmaceutically acceptable adjuvant is a phospholipid and an antioxidant.
Claim 22
Dependent Claim
26 words
The antitumorous composition according to Claim 15, wherein at least 80% of the benzoyl urea compound has a particle size of not larger than 5 µm.
Claim 23
Dependent Claim
18 words
The antitumorous composition according to Claim 15, which is applied for oral administration, intravenous administration or suppository administration.
Claim 24
Dependent Claim
13 words
The antitumorous composition according to Claim 15, which is applied for oral administration.
Claim 25
Independent Claim
24 words
A method for treating a cancer with a benzoyl urea compound having the formula: wherein A is a bromine atom or a chlorine atom.
Claim 26
Independent Claim
24 words
A method for treating a cancer with a benzoyl urea compound having the formula: wherein A is a bromine atom or a chlorine atom.
Claim 27
Dependent Claim
25 words
The method according to Claim 22, wherein the benzoyl urea compound is administered by oral administration, intravenous administration or suppository administration for curing the cancer.
Claim 28
Dependent Claim
16 words
The method according to Claim 22, wherein the benzoyl urea compound is administered by oral administration.
Claim 29
Dependent Claim
31 words
A pyrimidinyloxy benzene compound as an intermediate having the formula: wherein A is a bromine atom or a chlorine atom, and R 3 is an amino group or an isocyanate group.
Claim 30
Dependent Claim
31 words
A pyrimidinyloxy benzene compound as an intermediate having the formula: wherein A is a bromine atom or a chlorine atom, and R 3 is an amino group or an isocyanate group.
Claim 31
Dependent Claim
13 words
The compound according to Claim 25, wherein R 3 is an amino group.
Claim 32
Dependent Claim
9 words
The compound according to Claim 25, which is 4-(5-bromo-2-pyrimidinyloxy)-3-chloroaniline.
Claim 33
Dependent Claim
13 words
The compound according to Claim 25, wherein R 3 is an isocyanate group.
Claim 34
Dependent Claim
10 words
The compound according to Claim 25, which is 4-(5-bromo-2-pyrimidinyloxy)-3-chlorophenyl isocyanate.
Claim 35
Dependent Claim
4 words
N-(2-nitrobenzoyl)-N'-(3-chloro-4-hydroxyphenyl)urea as an intermediate.
Claim 36
Dependent Claim
4 words
N-(2-nitrobenzoyl)-N'-(3-chloro-4-hydroxyphenyl)urea as an intermediate.
References Cited (Backward Citations)
US435617A
Cited
EP0123861A2
Cited
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