Patent US4241053A successfully refreshed from Google Patents.
US4241053A
Expired / Lapsed
US
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Novel nitrosourea compounds and process for preparing the same
Assignee: Tanabe Pharma Corp
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Filing: 1979-08-14
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Granted: 1980-12-23
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Expires: 1999-08-14
Abstract
Abstract A compound of the formula: <IMAGE> wherein R1 is lower alkoxy, lower alkoxy-methoxy or 2-hydroxy-ethoxy, R2 is aldo-pentofuranosyl, aldo-pentopyranosyl, aldohexopyranosyl or O-aldo-hexopyranosyl-(1->4)-aldo-hexopyranosyl, and A is straight or branched alkylene of one to four carbon atoms, said alkylene being substituted with from 0 to at least one lower alkoxy group, is disclosed. A new intermediate used in the preparation of this compound is also disclosed. The end products are useful for inhibiting the growth of malignant tumor cells in warm-blooded animals; especially Leukemia and Ejrlich ascites carcinoma. Effectiveness on human beings has not yet been demonstrated.
Inventors
- 👤 Kenji Tsujihara
- 👤 Masakatsu Ozeki
- 👤 Yoshihisa Arai
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-01 19:19
CPC Classifications
C; C07; C07H; C07H13/00; C07H13/12
Claims Analysis
Total Claims: 22
Claim 1
Independent Claim
51 words
A compound of the formula: ##STR7## wherein R 1 is lower alkoxy, lower alkoxy-methoxy or 2-hydroxyethoxy, R 2 is aldo-pentofuranosyl, aldo-pentopyranosyl, aldo-hexopyranosyl or O-aldo-hexopyranosyl-(1→4)-aldo-hexopyranosyl, and A is straight or branched alkylene of one to four carbon atoms, said alkylene being substituted with from 0 to at least one lower alkoxy group.
Claim 2
Dependent Claim
51 words
A compound of the formula: ##STR7## wherein R 1 is lower alkoxy, lower alkoxy-methoxy or 2-hydroxyethoxy, R 2 is aldo-pentofuranosyl, aldo-pentopyranosyl, aldo-hexopyranosyl or O-aldo-hexopyranosyl-(1→4)-aldo-hexopyranosyl, and A is straight or branched alkylene of one to four carbon atoms, said alkylene being substituted with from 0 to at least one lower alkoxy group.
Claim 3
Dependent Claim
19 words
The compound of claim 1, in which R 2 is D-ribofuranosyl, L-arabinopyranosyl, D-arabinopyranosyl, D-xylopyranosyl, D-glucopyranosyl, D-galactopyranosyl, D-mannopyranosyl or O-α-D-glucopyranosyl-(1→4)-D-glucopyranosyl.
Claim 4
Dependent Claim
17 words
The compound of claim 2, in which R 1 is alkoxy of one or two carbon atoms.
Claim 5
Dependent Claim
19 words
The compound of claim 3, in which A is straight or branched alkylene of two or three carbon atoms.
Claim 6
Dependent Claim
18 words
The compound of claim 4, in which R 2 is D-ribofuranosyl, L-arabinopyranosyl, D-arabinopyranosyl, D-xylopyranosyl, D-galactopyranosyl, D-mannopyranosyl or O-α-D-glucopyranosyl-(1→4)-D-glucopyranosyl.
Claim 7
Dependent Claim
22 words
The compound of claim 4, in which R 2 is L-arabinopyranosyl, D-arabinopyranosyl or O-α-D-glucopyranosyl-(1→4)-D-glucopyranosyl, and A is ethylene, propylene, 1-methylethylene or 2-methylethylene.
Claim 8
Dependent Claim
14 words
The compound of claims 5 or 6, in which A is ethylene or propylene.
Claim 9
Dependent Claim
14 words
The compound of claims 5 or 6, in which A is 1-methylethylene or 2-methylethylene.
Claim 10
Dependent Claim
11 words
The compound of claim 6, in which R 1 is methoxy.
Claim 11
Dependent Claim
12 words
The compound of claim 9, in which A is ethylene or propylene.
Claim 12
Dependent Claim
12 words
The compound of claim 9, in which A is 1-methylethylene or 2-methylethylene.
Claim 13
Dependent Claim
8 words
The compound of claim 10 which is 1-(2-chloroethyl)-1-nitroso-3-(2-methoxyethyl)-3-(L-arabinopyranosyl)urea.
Claim 14
Dependent Claim
8 words
The compound of claim 10 which is 1-(2-chloroethyl)-1-nitroso-3-(3-methoxy-n-propyl)-3-(L-arabinopyranosyl)urea.
Claim 15
Dependent Claim
8 words
The compound of claim 10 which is 1-(2-chloroethyl)-1-nitroso-3-(3-methoxy-n-propyl)-3-(D-arabinopyranosyl)-urea.
Claim 16
Dependent Claim
8 words
The compound of claim 11 which is 1-(2-chloroethyl)-1-nitroso-3-(2-methoxy-n-propyl)-3-[O-α-D-glucopyranosyl-(1→4)-D-glucopyranosyl]urea.
Claim 17
Dependent Claim
8 words
The compound of claim 11 which is 1-(2-chloroethyl)-1-nitroso-3-(1-methyl-2-methoxy-ethyl)-3-[O-α-D-glucopyranosyl-(1→4)-D-glucopyranosyl]urea.
Claim 18
Dependent Claim
8 words
The compound of claim 11 which is 1-(2-chloroethyl)-1-nitroso-3-(2-methoxy-n-propyl)-3-(L-arabinopyranosyl)-urea.
Claim 19
Dependent Claim
8 words
The compound of claim 11 which is 1-(2-chloroethyl)-1-nitroso-3-(1-methyl-2-methoxy-ethyl)-3-(L-arabinopyranosyl)urea.
Claim 20
Dependent Claim
51 words
A compound of the forumula: ##STR8## wherein R 1 is lower alkoxy, lower alkoxy-methoxy or 2-hydroxyethoxy, R 2 is aldo-pentofuranosyl, aldo-pentopyranosyl, aldo-hexopyranosyl or O-aldo-hexopyranosyl(1→4)-aldo-hexopyranosyl, and A is straight or branched alkylene of one to four carbon atoms, said alkylene being substituted with from 0 to at least one lower alkoxy group.
Claim 21
Dependent Claim
51 words
A compound of the forumula: ##STR8## wherein R 1 is lower alkoxy, lower alkoxy-methoxy or 2-hydroxyethoxy, R 2 is aldo-pentofuranosyl, aldo-pentopyranosyl, aldo-hexopyranosyl or O-aldo-hexopyranosyl(1→4)-aldo-hexopyranosyl, and A is straight or branched alkylene of one to four carbon atoms, said alkylene being substituted with from 0 to at least one lower alkoxy group.
Claim 22
Dependent Claim
20 words
A therapeutic composition which comprises a therapeutically effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1983-12-23 | 1984-06-23 | 1984-12-23 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-12-23 | 1988-06-23 | 1988-12-23 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-12-23 | 1992-06-23 | 1992-12-23 | $7700.00 | Window Closed / Lapsed |