US4558047A
Expired / Lapsed
US
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3,5-Di hydroxy morpholine derivatives and pharmaceutical compositions
Assignee: Astellas Pharma Inc
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Filing: 1984-04-10
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Granted: 1985-12-10
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Expires: 2004-04-10
Abstract
Abstract 3,5-Di hydroxy morpholine derivatives having antitumor activity and methods of preparation thereof, are disclosed.
Inventors
- 👤 Takao Takaya
- 👤 Zenzaburo Tozuka
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 22:47
CPC Classifications
C; C07; C07D; C07D473/00; A; A61; A61P; A61P35/00; C07D265/00; C07D265/28; C07D265/30; C07D265/32; C07D413/00; C07D413/14; C07D417/00; C07D417/14; C07H; C07H19/00; C07H19/02; C07H19/04
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
62 words
A compound of the formula: ##STR20## wherein R 1 is a heterocyclic group selected from uracilyl, cytosinyl, hypoxanthinyl, adeninyl and thiazolyl, which may be substituted with halogen or carbamoyl, R 2 is an N-containing unsaturated heterocyclic group which may be substituted with oxo or lower alkyl, and R 3 is a hydrogen atom or a phosphono group, and pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
62 words
A compound of the formula: ##STR20## wherein R 1 is a heterocyclic group selected from uracilyl, cytosinyl, hypoxanthinyl, adeninyl and thiazolyl, which may be substituted with halogen or carbamoyl, R 2 is an N-containing unsaturated heterocyclic group which may be substituted with oxo or lower alkyl, and R 3 is a hydrogen atom or a phosphono group, and pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
40 words
A compound of claim 1, wherein R 2 is an N-containing unsaturated heterocyclic group selected from 5 membered ring, 6 membered ring and fused ring comprising 5 and 6 membered rings, which may be substituted with oxo or lower alkyl.
Claim 4
Dependent Claim
27 words
A compound of claim 2, wherein R 2 is an N-containing unsaturated heterocyclic group selected from thiadiazolyl, thiazolyl, thiazolinyl, isoxazolyl, pyrazolyl, triazolyl, tetrazolyl, pyrimidinyl, purinyl and hypoxanthinyl.
Claim 5
Dependent Claim
16 words
A compound of claim 3, wherein R 2 is thiadiazolyl, thiazolyl, tetrazolyl, pyrimidinyl, purinyl or hypoxanthinyl.
Claim 6
Dependent Claim
24 words
A compound of claim 4, wherein R 1 is uracilyl, cytosinyl, hypoxanthinyl, thiazolyl, in which these groups may be substituted with halogen or carbamoyl.
Claim 7
Dependent Claim
14 words
A compound of claim 5, wherein R 1 is uracilyl optionally substituted with halogen.
Claim 8
Dependent Claim
9 words
A compound of claim 6, which is 1-[(2R, 6R)-3,5-dihydroxy-6-hydroxymethyl-4-(2-pyrimidinyl)morpholin-2-yl]uracil.
Claim 9
Dependent Claim
9 words
A compound of claim 6, which is 1-[(2R, 6R)-3,5-dihydroxy-6-hydroxymethyl-4-(1,2,4-triazol-3-yl)morpholin-2-yl]uracil.
Claim 10
Dependent Claim
9 words
A compound of claim 6, which is 1-[(2R, 6R)-3,5-dihydroxy-6-hydroxymethyl-4-(1,3,4-thiadiazol-2-yl)morpholin-2-yl]uracil.
Claim 11
Dependent Claim
14 words
A compound of claim 5, wherein R 1 is cytosinyl optionally substituted with halogen.
Claim 12
Dependent Claim
9 words
A compound of claim 10, which is 1-[(2R, 6R)-3,5-dihydroxy-6-hydroxymethyl-4-(2-pyrimidinyl)morpholin-2-yl]cytosine
Claim 13
Dependent Claim
9 words
A compound of claim 10, which is 1-[(2R, 6R)-3,5-dihydroxy-6-hydroxymethyl-4-(2-pyrimidinyl)morpholin-2-yl]-5-fluorocytosine.
Claim 14
Dependent Claim
14 words
A compound of claim 5, wherein R 1 is thiazolyl optionally substituted with carbamoyl.
Claim 15
Dependent Claim
9 words
A compound of claim 13, which is 2-[(2R, 6R)-3,5-dihydroxy-6-hydroxymethyl-4-(2-pyrimidinyl)morpholin-2-yl]-4-carbamoylthiazole.
Claim 16
Dependent Claim
10 words
A compound of claim 5, wherein R 1 is hypoxanthinyl.
Claim 17
Dependent Claim
9 words
A compound of claim 15, which is 9-[(2R, 6R)-3,5-dihydroxy-6-hydroxymethyl-4-(6-purinyl)morpholin-2-yl]hypoxanthine.
Claim 18
Dependent Claim
9 words
A compound of claim 15, which is 9-[(2R, 6R)-3,5-dihydroxy-6-hydroxymethyl-4-(2-hypoxanthinyl)morpholin-2-yl]hypoxanthine.
Claim 19
Dependent Claim
24 words
A pharmaceutical composition comprisng a compound of claim 1, as an effective ingredient, in association with a pharmaceutically acceptable, substantially nontoxic carrier or excipient.
References Cited (Backward Citations)
US3542776A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1988-12-09 | 1989-06-10 | 1989-12-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-12-09 | 1993-06-10 | 1993-12-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-12-09 | 1997-06-10 | 1997-12-10 | $7700.00 | Window Closed / Lapsed |