US4994443A
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US
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Inhibition of angiogenesis
Assignee: Boston Children's Hospital
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Filing: 1988-10-13
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Granted: 1991-02-19
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Expires: 2008-10-13
Abstract
Abstract Angiogenesis in mammals is inhibited by administration of the active agents (1) heparin or a heparin fragment which is a hexasaccharide or larger or analogous compounds and (2) a steroid having 17 alpha - and 21-hydroxy groups, 3- and 20-one groups, and in the 16-position hydrogen hydroxy or a methyl group, and non-toxic physiologically acceptable carboxylates, acetals, ketals and phosphates thereof.
Inventors
- 👤 Moses J. Folkman
- 👤 Stephanie Taylor
- 👤 Robert S. Langer
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 01:31
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/70; A61K31/715
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
139 words
A composition for treating mammals for stopping growth, bringing about regression, or preventing metastasis of solid tumors in mammals by oral, or parenteral administration in which the active agents consist essentially of effective proportions for said treating of (1) a member selected from the group consisting of a said composition including a non-toxic physiologically acceptable carrier adapted for oral or parenteral administration, said composition exhibiting an avascular zone when implanted in an immature chick chorioallantoic membrane. heparin fragment which is either a hexasaccharide or larger oligosaccharide and an analogous compound having of the structures ##STR2## and (2) a member selected from the group consisting of steroids having a 17α- and 21-hydroxy groups, 3- and 20-one groups, and in the 16-position hydrogen, hydroxy, or a methyl group, and a non-toxic physiologically acceptable carboxylate, or acetal, or ketal, or phosphate thereof.
Claim 2
Dependent Claim
139 words
A composition for treating mammals for stopping growth, bringing about regression, or preventing metastasis of solid tumors in mammals by oral, or parenteral administration in which the active agents consist essentially of effective proportions for said treating of (1) a member selected from the group consisting of a said composition including a non-toxic physiologically acceptable carrier adapted for oral or parenteral administration, said composition exhibiting an avascular zone when implanted in an immature chick chorioallantoic membrane. heparin fragment which is either a hexasaccharide or larger oligosaccharide and an analogous compound having of the structures ##STR2## and (2) a member selected from the group consisting of steroids having a 17α- and 21-hydroxy groups, 3- and 20-one groups, and in the 16-position hydrogen, hydroxy, or a methyl group, and a non-toxic physiologically acceptable carboxylate, or acetal, or ketal, or phosphate thereof.
Claim 3
Dependent Claim
28 words
A composition as claimed in claim 1 in which the active agents consist essentially of a heparin fragment which is either a hexasaccharide or larger oligosaccharide and cortisone.
Claim 4
Dependent Claim
27 words
A composition as claimed in claim 1 in which the active agents consist essentially of a heparin fragment which is either hexasaccharide or larger oligosaccharide and hydrocortisone.
Claim 5
Dependent Claim
136 words
A composition for treating mammals for stopping growth, bringing about regression, or preventing metastasis of solid tumors in mammals by oral administration only, in which the active agents consist essentially of effective proportions for said treating of (1) a member selected from the group consisting of heparin and a heparin fragment which is either a hexasaccharide or larger oligosaccharide and an analogous compound having one of the structures ##STR3## and (2) a member selected from the group consisting of steroids having 17α- and 21-hydroxy groups, 3- and in the 16-position hydrogen, hydroxy, or a methyl group, and a non-toxic physiologically acceptable carboxylate, or acetal, or ketal, or phosphate thereof, said composition including a non-toxic physiologically acceptable carrier adapted for oral administration only. said composition exhibiting an avascular zone when implanted in an immature chick chorioallantoic membrane.
Claim 6
Dependent Claim
136 words
A composition for treating mammals for stopping growth, bringing about regression, or preventing metastasis of solid tumors in mammals by oral administration only, in which the active agents consist essentially of effective proportions for said treating of (1) a member selected from the group consisting of heparin and a heparin fragment which is either a hexasaccharide or larger oligosaccharide and an analogous compound having one of the structures ##STR3## and (2) a member selected from the group consisting of steroids having 17α- and 21-hydroxy groups, 3- and in the 16-position hydrogen, hydroxy, or a methyl group, and a non-toxic physiologically acceptable carboxylate, or acetal, or ketal, or phosphate thereof, said composition including a non-toxic physiologically acceptable carrier adapted for oral administration only. said composition exhibiting an avascular zone when implanted in an immature chick chorioallantoic membrane.
Claim 7
Dependent Claim
20 words
The composition as claimed in claim 4 in which the active agents consist essentially of (1) heparin and (2) cortisone.
Claim 8
Dependent Claim
20 words
The composition as claimed in claim 4 in which the active agents consist essentially of (1) heparin and (2) hydrocortisone.
Claim 9
Independent Claim
112 words
A method of treating mammals bearing solid tumor masses to stop growth, to bring about regression or to prevent metastasis thereof which comprises administering orally thereto a dose effective for said treating of active agents consisting essentially of (1) heparin or a heparin fragment which is a hexasaccharide or larger oligosaccharide or an analogous compound having one of the structures ##STR4## and (2) a steroid having 17 α- and 21-hydroxy groups, 3- and 20-one groups, and in the 16- position hydrogen, hydroxy, or a methyl group, and a non-toxic physiologically acceptable carboxylate, or acetal, or ketal, or phosphate thereof, wherein said tumor masses are susceptible to said treatment with said active agents.
Claim 10
Independent Claim
112 words
A method of treating mammals bearing solid tumor masses to stop growth, to bring about regression or to prevent metastasis thereof which comprises administering orally thereto a dose effective for said treating of active agents consisting essentially of (1) heparin or a heparin fragment which is a hexasaccharide or larger oligosaccharide or an analogous compound having one of the structures ##STR4## and (2) a steroid having 17 α- and 21-hydroxy groups, 3- and 20-one groups, and in the 16- position hydrogen, hydroxy, or a methyl group, and a non-toxic physiologically acceptable carboxylate, or acetal, or ketal, or phosphate thereof, wherein said tumor masses are susceptible to said treatment with said active agents.
Claim 11
Dependent Claim
22 words
The method as claimed in claim 7 in which administration is oral and the active agents consists essentially of heparin and hydrocortisone.
Claim 12
Dependent Claim
25 words
The method as claimed in claim 7 in which administration is oral and the active agents consist essentially of a hexasaccharide heparin fragment and hydrocortisone.
Claim 13
Dependent Claim
20 words
The method as claimed in claim 7 in which said administration is oral and said active agent (1) is heparin.
Claim 14
Independent Claim
110 words
A method of treating mammals bearing solid tumor masses to stop growth, to bring about regression or to prevent metastasis thereof which comprises administering thereto an effective dose effective for said treating of active agents consisting essentially of (1) a heparin fragment which is either a hexasaccharide or larger oligosaccharide or an analogous compound having one of the structures ##STR5## and (2) a steroid having 17α- and 21-hydroxy groups, 3- and 20-one groups, and in the 16- position hydrogen, hydroxy, or a methyl group, and a non-toxic physiologically acceptable carboxylate, or acetal, or ketal, or phosphate thereof, wherein said tumor masses are susceptible to said treatment with said active agents.
Claim 15
Independent Claim
110 words
A method of treating mammals bearing solid tumor masses to stop growth, to bring about regression or to prevent metastasis thereof which comprises administering thereto an effective dose effective for said treating of active agents consisting essentially of (1) a heparin fragment which is either a hexasaccharide or larger oligosaccharide or an analogous compound having one of the structures ##STR5## and (2) a steroid having 17α- and 21-hydroxy groups, 3- and 20-one groups, and in the 16- position hydrogen, hydroxy, or a methyl group, and a non-toxic physiologically acceptable carboxylate, or acetal, or ketal, or phosphate thereof, wherein said tumor masses are susceptible to said treatment with said active agents.
Claim 16
Dependent Claim
26 words
The method as claimed in claim 11 in which the active agents consist essentially of (1) either said heparin fragment or analogous compound and (2) cortisone.
Claim 17
Dependent Claim
22 words
The method as claimed in claim 11 in which the active agents consist essentially of (1) said heparin fragment and (2) cortisone.
Claim 18
Dependent Claim
26 words
The method as claimed in claim 11 in which the active agents consists essentially of (1) either said heparin fragment or analogous compound and (2) hydrocortisone.
Claim 19
Dependent Claim
22 words
The method as claimed in claim 11 in which said active agents consist essentially of (1) said heparin fragment and (2) hydrocortisone.
References Cited (Backward Citations)
US4771042A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1994-02-18 | 1994-08-20 | 1995-02-19 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1998-02-18 | 1998-08-20 | 1999-02-19 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2002-02-18 | 2002-08-20 | 2003-02-19 | $7700.00 | Window Closed / Lapsed |