EP0404525A2
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Sulfur-containing fused pyrimidine derivatives, their production and use
Assignee: Takeda Pharmaceutical Co Ltd
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Filing: 1990-06-19
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Granted: —
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Expires: 2010-06-19
Abstract
Abstract Disclosed is a compound represented by the formula (I) or a salt thereof: wherein R' represents an aliphatic hydrocarbon, aralkyl or aryl group which may be substituted; R 2 represents hydrogen, an aliphatic hydrocarbon group having one or more substituents, an aryl group which may be substituted, an amino group which may be substituted, a formyl group, a nitro group or a halogeno group; A represents a divalent hydrocarbon chain of 2 to 4 carbon atoms which may be substituted; and m represents an integer of 0 to 2, which is useful for treatment and prevention of diseases induced by abnormalities in regulation of reactions in vivo mediated through endothelin or interleukin 1, and of immune diseases and inflammatory diseases.
Inventors
- 👤 Takehiko Naka
- 👤 Taketoshi Saijo
- 👤 Norio Shimamoto
- 👤 Masahiro Suno
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-25 10:42
CPC Classifications
C; C07; C07D; C07D513/00; C07D513/02; C07D513/04; A; A61; A61P; A61P29/00; A61P37/00; A61P43/00; A61P9/00; A61P9/10
Claims Analysis
Total Claims: 17
Claim 1
Independent Claim
199 words
A production method of a compound represented by the formula (I) or a pharmacologically acceptable salt thereof: wherein R' represents an aliphatic hydrocarbon, aralkyl or aryl group which may be substituted; R 2 represents hydrogen, an aliphatic hydrocarbon group having one or more substituents, an aryl group which may be substituted, an amino group which may be substituted, a formyl group, a nitro group or a halogeno group; A represents a divalent hydrocarbon chain of 2 to 4 carbon atoms which may be substituted; and m represents an integer of 0 to 2, which method comprises reacting a compound of the formula (11): with a sulfur reagent in an organic solvent to obtain a compound of the formula (III): wherein R 3 represents hydrogen, an alkyl group which may be substituted, -YR 5 [wherein Y is -0- or -S-, and R 5 is hydrogen, a lower alkyl group of 1 to 4 carbon atoms or an aryl group which may be substituted], or a fatty acid-derived lower acyl group of 1 to 4 carbon atoms; R 4 represents hydrogen or a lower alkyl group of 1 to 4 carbon atoms; and n represents an integer of 0 to 2.
Claim 2
Dependent Claim
199 words
A production method of a compound represented by the formula (I) or a pharmacologically acceptable salt thereof: wherein R' represents an aliphatic hydrocarbon, aralkyl or aryl group which may be substituted; R 2 represents hydrogen, an aliphatic hydrocarbon group having one or more substituents, an aryl group which may be substituted, an amino group which may be substituted, a formyl group, a nitro group or a halogeno group; A represents a divalent hydrocarbon chain of 2 to 4 carbon atoms which may be substituted; and m represents an integer of 0 to 2, which method comprises reacting a compound of the formula (11): with a sulfur reagent in an organic solvent to obtain a compound of the formula (III): wherein R 3 represents hydrogen, an alkyl group which may be substituted, -YR 5 [wherein Y is -0- or -S-, and R 5 is hydrogen, a lower alkyl group of 1 to 4 carbon atoms or an aryl group which may be substituted], or a fatty acid-derived lower acyl group of 1 to 4 carbon atoms; R 4 represents hydrogen or a lower alkyl group of 1 to 4 carbon atoms; and n represents an integer of 0 to 2.
Claim 3
Dependent Claim
21 words
Production method according to claim 1, wherein a sufur reagent is NaSH, Na 2 S or (NH 4 ) 2 S.
Claim 4
Dependent Claim
48 words
Production method of a compound according to claim 1, which comprises reacting a compound of the formula (XXVIII): with a thioglycolic acid in the presence of a base in an organic solvent to obtain a compound of the formula (XXIX): wherein R 17 is hydrogen or lower alkyl
Claim 5
Dependent Claim
32 words
Production method according to claim 1 or 3, further comprising oxydation, nitration, reduction, hydrolysis, alkylation, formylation, halogenation, dehydroxylation, acetalation, thioacetalation, condensation, Witting reaction, Mannich reaction, amidation, nucleophilic substitution, dehydrochchlorination, elimination or dealkylation.
Claim 6
Dependent Claim
29 words
An endotheline inhibiting composition which contains an effective amount of a compound (I) as defined in claim 1 or a pharmaceutically acceptable salt thereof and pharmaceutically acceptable additional components.
Claim 7
Dependent Claim
29 words
An IL-1 inhibiting composition which contains an effective amount of a compound (I) as defined in claim I or a pharmaceutically acceptable salt thereof and pharmaceutically acceptable additional components.
Claim 8
Dependent Claim
29 words
An NGF stimulating composition which contains an effective amount of a compound (I) as defined in claim 1 or a pharmaceutically acceptable salt thereof and pharmaceutically acceptable additional components.
Claim 9
Dependent Claim
23 words
A composition according to claim 5, 6 or 7, wherein the pharmaceutically acceptable components include vehicle, disintegrator, lubricant, binder, dispersant, plasticizer or diluent.
Claim 10
Dependent Claim
30 words
Use of a compound (I) as defined in claim 1 or a pharmacologically acceptable salt thereof for the manufacture of a medicament for preventing the physiological role of endothelial action.
Claim 11
Dependent Claim
28 words
Use of a compound (I) as defined in claim 1 or a pharmacologically acceptable salt thereof for the manufacture of a medicament for preventing the production of IL-1.
Claim 12
Dependent Claim
28 words
Use of a compound (I) as defined in claim 9 or a pharmacologically acceptable salt thereof for the manufacture of a medicament for stimulating the production of NGF.
Claim 13
Dependent Claim
17 words
The use of a compound according to claim 9 wherein the said compound (I) is 9-phenyl-7-propyl-4H,6H-pyrimidino[6,1 -b][1,3]thiazine-6,8(7H)-dione.
Claim 14
Dependent Claim
17 words
The use of a compound according to claim 9 wherein the said compound (I) is 7-benzyl-9-phenyl-4H,6H-pyrimidino[6,1 -b][1,3]thiazine-6,8(7H)-dione.
Claim 15
Dependent Claim
17 words
The use of a compound according to claim 9 wherein the said compound (I) is 7-(p-chlorobenzyl)-9-phenyl-4H,6H-pyrimidino[6-1 -b][1,3]thiazine-6,8(7H-dione.
Claim 16
Dependent Claim
16 words
The use of a compound according to claim 9 wherein the said compound is 7-benzyl-9-phenyl-2H,6H-pyrimidino[6,1 -b][1,3]thiazine-6,8(7H)-dione.
Claim 17
Dependent Claim
16 words
The use of a compound according to claim 9 wherein the said compound is 9-phenyl-7-propyl-2H,6H-pyrimidino[6,1 -b][1,3]thiazine-6,8(7H)-dione.
References Cited (Backward Citations)
No citation records indexed.
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