EP0340905A1
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Fused pyrimidines, their production and use
Assignee: Takeda Pharmaceutical Co Ltd
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Filing: 1989-03-30
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Granted: —
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Expires: 2009-03-30
Abstract
Abstract New fused pyrimidines of the general formula (I): wherein the ring Ⓐ is a pyridine ring which may be hydrogenated or a benzene ring which may be hydrogenated, X is an amino group or a hydroxyl group, R¹, R², R³ and R⁴ are independently hydrogen, fluorine or a lower alkyl group, and -COOR⁵ and -COOR⁶ are independently a carboxyl group which may be esterified, and salts thereof have excellent anti-tumor effects, and they can be produced by the following reaction scheme: in which Ⓐ is , X, R¹ to R⁴, -COOR⁵ have the above meanings.
Inventors
- 👤 Hiroaki Nomura
- 👤 Hiroshi Akimoto
- 👤 Tetsuo Miwa
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-01 16:53
CPC Classifications
C; C07; C07D; C07D239/00; C07D239/70; C07D239/72; C07D471/00; C07D471/02; C07D471/04; A; A61; A61P; A61P35/00; C07D239/95
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
66 words
A compound of the general formula: wherein the ring Ⓐ is a pyridine ring which may be hydrogenated or a benzene ring which may be hydrogenated, X is an amino group or a hydroxyl group, R¹, R², R³ and R⁴ are independently hydrogen, fluorine or a lower alkyl group, and -COOR⁵ and -COOR⁶ are independently a carboxyl group which may be esterified, or a salt thereof.
Claim 2
Dependent Claim
66 words
A compound of the general formula: wherein the ring Ⓐ is a pyridine ring which may be hydrogenated or a benzene ring which may be hydrogenated, X is an amino group or a hydroxyl group, R¹, R², R³ and R⁴ are independently hydrogen, fluorine or a lower alkyl group, and -COOR⁵ and -COOR⁶ are independently a carboxyl group which may be esterified, or a salt thereof.
Claim 3
Dependent Claim
15 words
A compound as claimed in claim 1, wherein the ring Ⓐ is pyridine or tetrahydropyridine.
Claim 4
Dependent Claim
22 words
A compound as claimed in claim 1, wherein the lower alkyl group is an alkyl group having 1 to 3 carbon atoms.
Claim 5
Dependent Claim
75 words
A compound as claimed in claim 1, wherein the carboxyl group which may be esterified is a carboxyl group which may be esterified by a lower alkyl group having 1 to 5 carbon atoms, a benzyl group which may be substituted with nitro or a lower alkoxy group having 1 to 3 carbon atoms, or a phenyl group which may be substituted with nitro or a lower alkxoy group having 1 to 3 carbon atoms.
Claim 6
Dependent Claim
15 words
A compound as claimed in claim 1, wherein the salt is a pharmaceutically acceptable salt.
Claim 7
Dependent Claim
38 words
A compound as claimed in claim 1, which is a compound of the general formula: wherein X, R¹, R², R³, R⁴, R⁵ and R⁶ are the same as defined in claim 1, or a pharmaceutically acceptable salt thereof.
Claim 8
Dependent Claim
16 words
A compound as claimed in claim 6, wherein R², R³, R⁴, R⁵ and R⁶ are hydrogen.
Claim 9
Dependent Claim
21 words
A compound as claimed in claim 6, wherein R¹ is hydrogen or an alkyl group having 1 to 3 carbon atoms.
Claim 10
Dependent Claim
13 words
A compound as claimed in claim 6, wherein X is an amino group.
Claim 11
Dependent Claim
11 words
A compound as claimed in claim 1, which is N-[4-[3-(2,4-diamino-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidin-6-yl)propyl]benzoyl]-L-glutamic acid.
Claim 12
Dependent Claim
128 words
A process for producing a compound of the general formula: wherein the ring Ⓐ is a pyridine ring which may be hydrogenated or a benzene ring which may be hydrogenated, X is an amino group or a hydroxyl group, R¹, R², R³ and R⁴ are independently hydrogen, fluorine or a lower alkyl group, and -COOR⁵ and -COOR⁶ are independently a carboxyl group which may be esterified, or a salt thereof, which comprises reacting a compound of the general formula: wherein the ring Ⓐ, X, R¹, R², R³ and R⁴ are the same as defined before, or a reactive derivative at the carboxyl group or a salt thereof, with a compound of the general formula: wherein -COOR⁵ and -COOR⁶ are the same as defined before, or a salt thereof.
Claim 13
Dependent Claim
128 words
A process for producing a compound of the general formula: wherein the ring Ⓐ is a pyridine ring which may be hydrogenated or a benzene ring which may be hydrogenated, X is an amino group or a hydroxyl group, R¹, R², R³ and R⁴ are independently hydrogen, fluorine or a lower alkyl group, and -COOR⁵ and -COOR⁶ are independently a carboxyl group which may be esterified, or a salt thereof, which comprises reacting a compound of the general formula: wherein the ring Ⓐ, X, R¹, R², R³ and R⁴ are the same as defined before, or a reactive derivative at the carboxyl group or a salt thereof, with a compound of the general formula: wherein -COOR⁵ and -COOR⁶ are the same as defined before, or a salt thereof.
Claim 14
Dependent Claim
63 words
A compound of the general formula: wherein the ring Ⓐ is a pyridine ring which may be hydrogenated or a benzene ring which may be hydrogenated, X is an amino group or a hydroxyl group, R¹, R², R³ and R⁴ are independently hydrogen, fluorine or a lower alkyl group, and -COOR⁷ is a carboxyl group which may be esterified, or a salt thereof.
Claim 15
Dependent Claim
63 words
A compound of the general formula: wherein the ring Ⓐ is a pyridine ring which may be hydrogenated or a benzene ring which may be hydrogenated, X is an amino group or a hydroxyl group, R¹, R², R³ and R⁴ are independently hydrogen, fluorine or a lower alkyl group, and -COOR⁷ is a carboxyl group which may be esterified, or a salt thereof.
Claim 16
Dependent Claim
84 words
An anti-tumor composition which contains an effective amount of a compound of the general formula: wherein the ring Ⓐ is a pyridine ring which may be hydrogenated or a benzene ring which may be hydrogenated, X is an amino group or a hydroxyl group, R¹, R², R³ and R⁴ are independently hydrogen, fluorine or a lower alkyl group, and -COOR⁵ and -COOR⁶ are independently a carboxyl group which may be esterified, or a salt thereof together with one or more carriers, diluents or excipients.
Claim 17
Dependent Claim
84 words
An anti-tumor composition which contains an effective amount of a compound of the general formula: wherein the ring Ⓐ is a pyridine ring which may be hydrogenated or a benzene ring which may be hydrogenated, X is an amino group or a hydroxyl group, R¹, R², R³ and R⁴ are independently hydrogen, fluorine or a lower alkyl group, and -COOR⁵ and -COOR⁶ are independently a carboxyl group which may be esterified, or a salt thereof together with one or more carriers, diluents or excipients.
Claim 18
Dependent Claim
28 words
The use of a compound (I) as defined in claim 1, or a pharmaceutically acceptable salt thereof in the preparation of a medicine for anti-tumor or cancer therapy.
References Cited (Backward Citations)
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