US4284074A
Expired / Lapsed
US
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IUD Arrangement
Assignee: Individual
•
Filing: 1979-07-09
•
Granted: 1981-08-18
•
Expires: 1999-07-09
Abstract
Abstract An intrauterine device of the type having an external surface contacting the walls of the uterus after insertion therein, and said device having first walls defining a fluid-receiving cavity in at least a portion thereof. A concentrated fluid solution of a drug is present in the cavity and the drug is of the type providing an antifibrinolytic, an antifertility and antiproteolytic effect and is one or a mixture of more than one guanidine such as any aromatic monoguanidine, aromatic diguanidine, non-aromatic monoguanidine and non-aromatic diguanidine, and mixtures of one or more of the guanidines with one or more amidines.
Inventors
- 👤 Seth T. Shaw, Jr.
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 12:07
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0034; A61K9/0039
Claims Analysis
Total Claims: 52
Claim 1
Independent Claim
121 words
In an intrauterine device of the type insertable in the uterus and having a surface contacting the uterus and first walls defining a fluid-receiving cavity in at least a portion thereof, the improvement comprising, in combination: one of a concentrated fluid solution and suspension of at least one drug in said cavity and said at least one drug of the type providing an antifibrinolytic, a reversible antifertility, and an antiproteolytic effect; and said first walls of said intrauterine device comprising a polymer having a predetermined permeability to said at least one drug; said at least one drug comprises at least a guanidine, and whereby, said predetermined permeability of said first walls controls the release rate of said drug from said cavity.
Claim 2
Dependent Claim
121 words
In an intrauterine device of the type insertable in the uterus and having a surface contacting the uterus and first walls defining a fluid-receiving cavity in at least a portion thereof, the improvement comprising, in combination: one of a concentrated fluid solution and suspension of at least one drug in said cavity and said at least one drug of the type providing an antifibrinolytic, a reversible antifertility, and an antiproteolytic effect; and said first walls of said intrauterine device comprising a polymer having a predetermined permeability to said at least one drug; said at least one drug comprises at least a guanidine, and whereby, said predetermined permeability of said first walls controls the release rate of said drug from said cavity.
Claim 3
Dependent Claim
12 words
The arrangement defined in claim 1 wherein: said first walls are semi-flexible.
Claim 4
Dependent Claim
14 words
The arrangement defined in claim 1 wherein: said first walls define an inflatable cavity.
Claim 5
Dependent Claim
75 words
The arrangement defined in claim 1 wherein: said at least one drug is selected from the class consisting of: (a) a mixture of an amidine and a guanidine; (b) a mixture of more than one amidine and a guanidine; (c) a mixture of an amidine and more than one guanidine; (d) a mixture of more than one amidine and more than one guanidine; (e) a guanidine; and (f) a mixture of more than one guanidine.
Claim 6
Dependent Claim
35 words
The arrangement defined in claim 1 wherein: said guanidine of said at least one drug is selected from the class consisting of: (a) aromatic monoguanidines; (b) aromatic diguanidines; (c) non-aromatic monoguanidines; and (d) non-aromatic diguanidines.
Claim 7
Dependent Claim
148 words
The arrangement defined in claim 1 wherein: said at least one drug is selected from the class of aromatic monoguanidines of the group: ##STR19## wherein R is selected from the class consisting of: (a) a carbon chain free of other elements; (b) a carbon chain with at least one other element; (c) an aromatic group free of additional carbon atoms, carbon chains and other elements; (d) an aromatic group with at least one addition selected from the class consisting of carbon atoms, carbon chains and other elements; (e) a cyclic non-aromatic group free of additional carbon atoms, carbon chains and other elements; (f) a cyclic non-aromatic group with at least one addition selected from the class consisting of carbon atoms, carbon chains, and other elements; and (g) a combination of at least two of (a), (b), (c), (d), (e) and (f); and wherein: ##STR20## represents the benzene ring.
Claim 8
Dependent Claim
48 words
The arrangement defined in claim 1 wherein: said at least one drug is selected from the class of aromatic diguanidines of the group: ##STR21## and wherein each guanidine group ##STR22## is in one of a meta or para position with respect to R 1 , and in which:
Claim 9
Dependent Claim
47 words
R 1 is selected from the class consisting of: (a) a hydrocarbon chain free of ether and ester bonds to the benzene ring; and (b) a hydrocarbon chain having at least one bond selected from the class of ether bonds and ester bonds to the benzene ring;
Claim 10
Dependent Claim
47 words
R 1 is selected from the class consisting of: (a) a hydrocarbon chain free of ether and ester bonds to the benzene ring; and (b) a hydrocarbon chain having at least one bond selected from the class of ether bonds and ester bonds to the benzene ring;
Claim 11
Dependent Claim
27 words
R 2 and R 3 are selected from the class consisting of: hydrogen, chlorine, bromine, iodine, hydroxyl group and alkyl group; and ##STR23## represents the benzene ring.
Claim 12
Dependent Claim
27 words
R 2 and R 3 are selected from the class consisting of: hydrogen, chlorine, bromine, iodine, hydroxyl group and alkyl group; and ##STR23## represents the benzene ring.
Claim 13
Dependent Claim
102 words
The arrangement defined in claim 1 wherein: said at least one drug is selected from the class of nonaromatic monoguanidines of the group: ##STR24## wherein R is selected from the class consisting of: (a) a carbon chain free of other elements; (b) a carbon chain with at least one other element; (c) a cyclic non-aromatic group free of additional carbon atoms, carbon chains and other elements; (d) a cyclic non-aromatic group with at least one addition selected from the class consisting of carbon atoms, carbon chains and other elements; (e) a combination of at least two of (a), (b), (c), and (d).
Claim 14
Dependent Claim
103 words
The arrangement defined in claim 1 wherein: said at least one drug is selected from the class consisting of non-aromatic diguanidines of the group: ##STR25## wherein R is selected from the class consisting of: (a) a carbon chain free of other elements; (b) a carbon chain with at least one other element; (c) a cyclic non-aromatic group free of additional carbon atoms, carbon chains and other elements; (d) a cyclic non-aromatic group with at least one addition selected from the class consisting of carbon atoms, carbon chains and other elements; (e) a combination of at least two of (a), (b), (c), and (d).
Claim 15
Dependent Claim
20 words
The arrangement defined in claim 1 wherein said at least one drug is selected from the class consisting of: ##STR26##
Claim 16
Dependent Claim
61 words
The arrangement defined in claim 1 and further comprising: a coating on at least a portion of said surface of said intrauterine device, and said coating comprising one of a biodegradable cross-linked polymer and co-polymer of a second drug, and said second drug comprises at least a guanidine, and said second drug chemically bonded to said first portion of said surface.
Claim 17
Dependent Claim
16 words
The arrangement defined in claim 11 wherein: said second drug further comprises a soft hydrogel coating.
Claim 18
Dependent Claim
73 words
The arrangement defined in claim 11 wherein: said second drug is selected from the class consisting of: (a) a mixture of an amidine and a guanidine; (b) a mixture of more than one amidine and a guanidine; (c) a mixture of an amidine and more than one guanidine; (d) a mixture of more than one amidine and more than one guanidine; (e) a guanidine; and (f) a mixture of more than one guanidine.
Claim 19
Dependent Claim
35 words
The arrangement defined in claim 11 wherein: said guanidine of said at least one drug is selected from the class consisting of: (a) aromatic monoguanidines; (b) aromatic diguanidines; (c) non-aromatic monoguanidines; and (d) non-aromatic diguanidines.
Claim 20
Dependent Claim
153 words
The arrangement defined in claim 11 wherein: said at least a guanidine of said second drug is selected from the class consisting of aromatic monoguanidines of the group: ##STR27## wherein R is selected from the class consisting of: (a) a carbon chain free of other elements; (b) a carbon chain with at least one other element; (c) an aromatic group free of additional carbon atoms, carbon chains and other elements; (d) an aromatic group with at least one addition selected from the class consisting of carbon atoms, carbon chains and other elements; (e) a cyclic non-aromatic group free of additional carbon atoms, carbon chains and other elements; (f) a cyclic non-aromatic group with at least one addition selected from the class consisting of carbon atoms, carbon chains, and other elements; and (g) a combination of at least two of (a), (b), (c), (d), (e) and (f); and wherein: ##STR28## represents the benzene ring.
Claim 21
Dependent Claim
128 words
The arrangement defined in claim 11 wherein: said at least a guanidine of said second drug is selected from the class consisting of aromatic diguanidines of the group: ##STR29## and wherein each guanidine group ##STR30## is in one of a meta or para position with respect to R 1 , and in which: R 1 is selected from the class consisting of: (a) a hydrocarbon chain free of ether and ester bonds to the benzene ring; and (b) a hydrocarbon chain free of ether and ester bonds selected from the class of ether bonds and ester bonds to the benzene ring; R 2 and R 3 are selected from the class consisting of: hydrogen, chlorine, bromine, iodine, hydroxyl group and alkyl group; and ##STR31## represents the benzene ring.
Claim 22
Dependent Claim
108 words
The arrangement defined in claim 11 wherein said at least a guanidine of said second drug is selected from the class consisting of non-aromatic monoguanidines of the group: ##STR32## wherein R is selected from the class consisting of : (a) a carbon chain free of other elements; (b) a carbon chain with at least one other element; (c) a cyclic non-aromatic group free of additional carbon atoms, carbon chains and other elements; (d) a cyclic non-aromatic group with at least one addition selected from the class consisting of carbon atoms, carbon chains and other elements; (e) a combination of at least two of (a), (b), (c), and (d).
Claim 23
Dependent Claim
104 words
The arrangement defined in claim 11 wherein: said at least a guandine of said second drug is selected from the class consisting of the group: ##STR33## wherein R is selected from the class consisting of: (a) a carbon chain free of other elements; (b) a carbon chain with at least one other element; (c) a cyclic non-aromatic group free of additional carbon atoms, carbon chains and other elements; (d) a cyclic non-aromatic group with at least one addition selected from the class consisting of carbon atoms, carbon chains and other elements; (e) a combination of at least two of (a), (b), (c), and (d).
Claim 24
Dependent Claim
26 words
The arrangement defined in claim 11 wherein: said at least a guanidine of said second drug is selected from the class consisting of the group: ##STR34##
Claim 25
Dependent Claim
51 words
The arrangement defined in claim 1 and further comprising: a coating on at least a first portion of said surface of said intrauterine device, and said coating comprising one of a non-biodegradable monomer, dimer, oligomer and cross-linked polymer of a second drug, and said second drug comprises at least a guanidine.
Claim 26
Dependent Claim
73 words
The arrangement defined in claim 15 wherein: said second drug is selected from the class consisting of: (a) a mixture of an amidine and a guanidine; (b) a mixture of more than one amidine and a guanidine; (c) a mixture of an amidine and more than one guanidine; (d) a mixture of more than one amidine and more than one guanidine; (e) a guanidine; and (f) a mixture of more than one guanidine.
Claim 27
Dependent Claim
37 words
The arrangement defined in claim 15 and further comprising: said guanidine of said at least one drug is selected from the class consisting of: (a) aromatic monoguanidines; (b) aromatic diguanidines; (c) non-aromatic monoguanidines; and (d) non-aromatic diguanidines.
Claim 28
Dependent Claim
152 words
The arrangement defined in claim 15 wherein: said at least a guanidine of said second drug is selected from the class consisting of aromatic monoguanidines of the group: ##STR35## wherein R is selected from the class consisting of: (a) a carbon chain free of other elements; (b) a carbon chain with at least one other element; (c) an aromatic group free of additional carbon atoms, carbon chains and other elements; (d) an aromatic group with at least one addition selected from the class consisting of carbon atoms, carbon chains and other elements; (e) a cyclic non-aromatic group free of additional carbon atoms, carbon chains and other elements; (f) a cyclic non-aromatic group with at least one addition selected from the class consisting of carbon atoms, carbon chains, and other elements; and (g) a combination of at least two of (a), (b), (c), (d), (e) and (f); and ##STR36## represents the benzene ring.
Claim 29
Dependent Claim
128 words
The arrangement defined in claim 11 wherein: said at least a guanidine of said second drug is selected from the class consisting of aromatic diguanidines of the group: ##STR37## and wherein each guanidine group ##STR38## is in one of a meta or para position with respect to R 1 , and in which: R 1 is selected from the class consisting of: (a) a hydrocarbon chain free of ether and ester bonds to the benzene ring; and (b) a hydrocarbon chain free of ether and ester bonds selected from the class of ether bonds and ester bonds to the benzene ring; R 2 and R 3 are selected from the class consisting of: hydrogen, chlorine, bromine, iodine, hydroxyl group and alkyl group; and ##STR39## represents the benzene ring.
Claim 30
Dependent Claim
107 words
The arrangement defined in claim 15 wherein said at least a guanidine of said second drug is selected from the class consisting of non-aromatic monoguanidines of the group: ##STR40## wherein R is selected from the class consisting of: (a) a carbon chain free of other elements; (b) a carbon chain with at least one other element; (c) a cyclic non-aromatic group free of additional carbon atoms, carbon chains and other elements; (d) a cyclic non-aromatic group with at least one addition selected from the class consisting of carbon atoms, carbon chains and other elements; (e) a combination of at least two of (a), (b), (c), and (d).
Claim 31
Dependent Claim
104 words
The arrangement defined in claim 15 wherein: said at least a guanidine of said second drug is selected from the class consisting of the group: ##STR41## wherein R is selected from the class consisting of: (a) a carbon chain free of other elements; (b) a carbon chain with at least one other element; (c) a cyclic non-aromatic group free of additional carbon atoms, carbon chains and other elements; (d) a cyclic non-aromatic group with at least one addition selected from the class consisting of carbon atoms, carbon chains and other elements; (e) a combination of at least two of (a), (b), (c), and (d).
Claim 32
Dependent Claim
26 words
The arrangement defined in claim 15 wherein: said at least a guanidine of said second drug is selected from the class consisting of the group: ##STR42##
Claim 33
Dependent Claim
19 words
The arrangement defined in claim 11 further comprising: a coating of copper on a second portion of said surface.
Claim 34
Dependent Claim
19 words
The arrangement defined in claim 15 further comprising: a coating of copper on a second portion of said surface.
Claim 35
Dependent Claim
116 words
In an intrauterine device of the type insertable in the uterus and having a surface contacting the uterus and first walls defining a fluid receiving cavity in at least a portion thereof, the improvement comprising, in combination: one of a crystalline form and a paste form of at least one drug in said cavity and said drug of the type providing an anti-fibrinolytic, reversible anti-fertility, and an anti-proteolytic effect, and said at least one drug comprising at least a guanidine, and said first walls of said intrauterine device comprising a polymer having a predetermined permeability to said drug, whereby said predetermined permeability of said first walls controls the release rate of said drug from said cavity.
Claim 36
Dependent Claim
116 words
In an intrauterine device of the type insertable in the uterus and having a surface contacting the uterus and first walls defining a fluid receiving cavity in at least a portion thereof, the improvement comprising, in combination: one of a crystalline form and a paste form of at least one drug in said cavity and said drug of the type providing an anti-fibrinolytic, reversible anti-fertility, and an anti-proteolytic effect, and said at least one drug comprising at least a guanidine, and said first walls of said intrauterine device comprising a polymer having a predetermined permeability to said drug, whereby said predetermined permeability of said first walls controls the release rate of said drug from said cavity.
Claim 37
Dependent Claim
75 words
The arrangement defined in claim 30 wherein: said at least one drug is selected from the class consisting of: (a) a mixture of an amidine and a guanidine; (b) a mixture of more than one amidine and a guanidine; (c) a mixture of an amidine and more than one guanidine; (d) a mixture of more than one amidine and more than one guanidine; (e) a guanidine; and (f) a mixture of more than one guanidine.
Claim 38
Dependent Claim
35 words
The arrangement defined in claim 30 wherein: said guanidine of said at least one drug is selected from the class consisting of: (a) aromatic monoguanidines; (b) aromatic diguanidines; (c) non-aromatic monoguanidines; and (d) non-aromatic diguanidines.
Claim 39
Dependent Claim
148 words
The arrangement defined in claim 30 wherein: said at least one drug is selected from the class of aromatic monoguanidines of the group: ##STR43## wherein R is selected from the class consisting of: (a) a carbon chain free of other elements; (b) a carbon chain with at least one other element; (c) an aromatic group free of additional carbon atoms, carbon chains and other elements; (d) an aromatic group with at least one addition selected from the class consisting of carbon atoms, carbon chains and other elements; (e) a cyclic non-aromatic group free of additional carbon atoms, carbon chains and other elements; (f) a cyclic non-aromatic group with at least one addition selected from the class consisting of carbon atoms, carbon chains, and other elements; and (g) a combination of at least two of (a), (b), (c), (d), (e) and (f); and wherein: ##STR44## represents the benzene ring.
Claim 40
Dependent Claim
122 words
The arrangement defined in claim 30 wherein: said at least one drug is selected from the class of aromatic diguanidines of the group: ##STR45## and wherein each guanidine group ##STR46## is in one of a meta or para position with respect to R 1 , and in which: R 1 is selected from the class consisting of: (a) a hydrocarbon chain free of ether and ester bonds to the benzene ring; and (b) a hydrocarbon chain having at least one bond selected from the class of ether bonds and ester bonds to the benzene ring; R 2 and R 3 are selected from the class consisting of: hydrogen, chlorine, bromine, iodine, hydroxyl group and alkyl group; and ##STR47## represents the benzene ring.
Claim 41
Dependent Claim
102 words
The arrangement defined in claim 30 wherein: said at least one drug is selected from the class of non-aromatic monoguanidines of the group: ##STR48## wherein R is selected from the class consisting of: (a) a carbon chain free of other elements; (b) a carbon chain with at least one other element; (c) a cyclic non-aromatic group free of additional carbon atoms, carbon chains and other elements; (d) a cyclic non-aromatic group with at least one addition selected from the class consisting of carbon atoms, carbon chains and other elements; (e) a combination of at least two of (a), (b), (c), and (d).
Claim 42
Dependent Claim
103 words
The arrangement defined in claim 30 wherein: said at least one drug is selected from the class consisting of non-aromatic diguanidines of the group: ##STR49## wherein R is selected from the class consisting of: (a) a carbon chain free of other elements; (b) a carbon chain with at least one other element; (c) a cyclic non-aromatic group free of additional carbon atoms, carbon chains and other elements; (d) a cyclic non-aromatic group with at least one addition selected from the class consisting of carbon atoms, carbon chains and other elements; (e) a combination of at least two of (a), (b), (c), and (d).
Claim 43
Dependent Claim
20 words
The arrangement defined in claim 30 wherein said at least one drug is selected from the class consisting of: ##STR50##
Claim 44
Dependent Claim
65 words
The arrangement defined in claim 30 and further comprising: a coating on at least a first portion of said surface of said intrauterine device, and said coating comprising one of a: biodegradable cross-linked polymer, a biodegradable cross-linked co-polymer, a non-biodegradable monomer, a non-biodegradable dimer, a non-biodegradable oligomer, and a non-biodegradable cross-linked polymer of a second drug, and said second drug comprises at least a guanidine.
Claim 45
Dependent Claim
73 words
The arrangement defined in claim 38 wherein: said second drug is selected from the class consisting of: (a) a mixture of an amidine and a guanidine; (b) a mixture of more than one amidine and a guanidine; (c) a mixture of an amidine and more than one guanidine; (d) a mixture of more than one amidine and more than one guanidine; (e) a guanidine; and (f) a mixture of more than one guanidine.
Claim 46
Dependent Claim
35 words
The arrangement defined in claim 38 wherein: said guanidine of said at least one drug is selected from the class consisting of: (a) aromatic monoguanidines; (b) aromatic diguanidines; (c) non-aromatic monoguanidines; and (d) non-aromatic diguanidines.
Claim 47
Dependent Claim
153 words
The arrangement defined in claim 38 wherein: said at least a guanidine of said second drug is selected from the class consisting of aromatic monoguanidines of the group: ##STR51## wherein R is selected from the class consisting of: (a) a carbon chain free of other elements; (b) a carbon chain with at least one other element; (c) an aromatic group free of additional carbon atoms, carbon chains and other elements; (d) an aromatic group with at least one addition selected from the class consisting of carbon atoms, carbon chains and other elements; (e) a cyclic non-aromatic group free of additional carbon atoms, carbon chains and other elements; (f) a cyclic non-aromatic group with at least one addition selected from the class consisting of carbon atoms, carbon chains, and other elements; and (g) a combination of at least two of (a), (b), (c), (d), (e) and (f); and wherein: ##STR52## represents the benzene ring.
Claim 48
Dependent Claim
128 words
The arrangement defined in claim 38 wherein: said at least a guanidine of said second drug is selected from the class consisting of aromatic diguanidines of the group: ##STR53## and wherein each guanidine group ##STR54## is in one of a meta or para position with respect to R 1 , and in which: R 1 is selected from the class consisting of: (a) a hydrocarbon chain free of ether and ester bonds to the benzene ring; and (b) a hydrocarbon chain free of ether and ester bonds selected from the class of ether bonds and ester bonds to the benzene ring; R 2 and R 3 are selected from the class consisting of: hydrogen, chlorine, bromine, iodine, hydroxyl group and alkyl group; and ##STR55## represents the benzene ring.
Claim 49
Dependent Claim
107 words
The arrangement defined in claim 38 wherein: said at least a guanidine of said second drug is selected from the class consisting of non-aromatic monoguanidines of the group: ##STR56## wherein R is selected from the class consisting of: (a) a carbon chain free of other elements; (b) a carbon chain with at least one other element; (c) a cyclic non-aromatic group free of additional carbon atoms, carbon chains and other elements; (d) a cyclic non-aromatic group with at least one addition selected from the class consisting of carbon atoms, carbon chains and other elements; (e) a combination of at least two of (a), (b), (c), and (d).
Claim 50
Dependent Claim
104 words
The arrangement defined in claim 38 wherein: said at least a guanidine of said second drug is selected from the class consisting of the group: ##STR57## wherein R is selected from the class consisting of: (a) a carbon chain free of other elements; (b) a carbon chain with at least one other element; (c) a cyclic non-aromatic group free of additional carbon atoms, carbon chains and other elements; (d) a cyclic non-aromatic group with at least one addition selected from the class consisting of carbon atoms, carbon chains and other elements; (e) a combination of at least two of (a), (b), (c), and (d).
Claim 51
Dependent Claim
26 words
The arrangement defined in claim 38 wherein: said at least a guanidine of said second drug is selected from the class consisting of the group: ##STR58##
Claim 52
Dependent Claim
19 words
The arrangement defined in claim 38 further comprising: a coating of copper on a second portion of said surface.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1984-08-17 | 1985-02-16 | 1985-08-18 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-08-17 | 1989-02-16 | 1989-08-18 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-08-17 | 1993-02-16 | 1993-08-18 | $7700.00 | Window Closed / Lapsed |