EP1099700A1
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Crystalline oxathiolane derivatives
Assignee: Glaxo Group Ltd
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Filing: 1992-06-02
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Granted: —
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Expires: 2012-06-02
Abstract
Abstract (-) cis -4-Amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidine-2-one in crystalline form, in particular as needle-shaped or bypyramidyl crystals, pharmaceutical formulations thereof, methods for their preparation and their use in medicine.
Inventors
- 👤 Paul Ravenscroft
- 👤 Tony Gordon Roberts
- 👤 Paul Evans
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-04 10:52
CPC Classifications
C; C07; C07D; C07D411/00; C07D411/02; C07D411/04; A; A61; A61P; A61P31/00; A61P31/12; A61P31/14; A61P31/18
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
6 words
(-)- cis -4-Amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one
in crystalline form.
Claim 2
Dependent Claim
10 words
(-)- cis -4-Amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one
in the form of needle shaped crystals.
Claim 3
Dependent Claim
20 words
The crystalline form as claimed in claim 1 or claim 2 having a melting
point of less than about 130°C.
Claim 4
Dependent Claim
19 words
The crystalline form as claimed in any one of claims 1 to 3 having a
melting point of 124-127°C.
Claim 5
Dependent Claim
28 words
The crystalline form as claimed in any one of claims 1 to 4 having an
endotherm with an onset temperature of 124-127°C in its differential
scanning calorimetry profile.
Claim 6
Dependent Claim
26 words
The crystalline form as claimed in any one of claims 1 to 5 having an
absorption band in its infra-red spectrum at about 1110 wave numbers.
Claim 7
Dependent Claim
12 words
(-)- cis -4-Amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one
in the crystalline form as shown in Figure 1.
Claim 8
Dependent Claim
16 words
(-)- cis -4-Amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one
in crystalline form and having an infra-red spectrum a shown in
Figure 3.
Claim 9
Independent Claim
21 words
A method for the preparation of (-)- cis -4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one
in crystalline form which
comprises crystallisation of the compound from aqueous solution.
Claim 10
Independent Claim
24 words
A method for the preparation of (-)- cis -4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one
in crystalline form which
comprises distillation of an aqueous solution of the compound with
propan-1-ol.
Claim 11
Dependent Claim
26 words
A pharmaceutical formulation comprising (-)- cis -4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one
in crystalline
form as claimed in any one of claims 1 to 8 and a pharmaceutically
acceptable carrier therefor
Claim 12
Dependent Claim
15 words
A pharmaceutical formulation as claimed in claim 11 in a form suitable
for oral administration.
Claim 13
Dependent Claim
19 words
A pharmaceutical formulation as claimed in claim 11 or claim 12 in the
form of a tablet or capsule.
References Cited (Backward Citations)
EP0382526A2
Cited
WO1991017159A1
Cited
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