US5614515A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Lazaroid-based compositions and method for preventing adhesion formation using the same
Assignee: University of Southern California
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Filing: 1994-11-17
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Granted: 1997-03-25
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Expires: 2014-11-17
Abstract
Abstract Compositions and method for the minimization or prevention of adhesion formation, whereby an effective amount of at least one lazaroid compound, preferably one of general formula I, is administered for a period of time sufficient to permit tissue repair. The compound of general formulae I or II is preferably administered in conjunction with a delivery vehicle (e.g., microcapsules, microspheres, biodegradable polymer films, lipid-based delivery systems such as liposomes and lipid foams, viscous instillates and absorbable mechanical barriers) useful for maintaining local concentrations of the compound at an effective level.
Inventors
- 👤 Kathleen E. Rodgers
- 👤 Gere S. diZerega
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 09:35
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/495; A61K31/505; A61K31/506; A61K31/496; A61K31/56; A61K31/58; A61P; A61P41/00; A61P43/00; A61P7/00; A61P7/02
Claims Analysis
Total Claims: 23
Claim 1
Independent Claim
31 words
A method for prevention of formation of adhesions between organ surfaces, comprising administering an effective amount of at least one lazaroid for a period of time sufficient to permit tissue repair.
Claim 2
Independent Claim
31 words
A method for prevention of formation of adhesions between organ surfaces, comprising administering an effective amount of at least one lazaroid for a period of time sufficient to permit tissue repair.
Claim 3
Dependent Claim
79 words
A method according to claim 1 wherein said lazaroid comprises a compound of general formula I: ##STR7## wherein R represents a formula: ##STR8## wherein R represents H or CH 3 ; R 1 represents formula Ia, as defined above, or formula IIa: ##STR9## wherein R 2 , R 3 , R 4 , and R 5 independently represent H or NR 6 R 7 wherein R 6 and R 7 independently represent H and C 1 -C 6 alkyl.
Claim 4
Dependent Claim
39 words
A method according to claim 2, wherein the lazaroid comprises: 2-[[4-(2,6-Di-1-pyrrolindinyl-4-pyrimidinyl)-1-piperazinyl] methyl]-3,4-dihydro-2,5,7,8-tetramethyl-2H-1-benzopyran-6-ol, dihydrochloride; (-)-2-[[4-(2,6-Di-1-pyrrolindinyl-4-pyrimidinyl)-1-piperazinyl] methyl]-3,4-dihydro-2,5,7,8-tetramethyl-2H-1-benzopyran-6-ol, 2-hydroxy-1,2,3-propanetricarboxylate; 2H-1-benzopyran-6-ol, 2-[[4-[3-(ethylamino)-2-pyridinyl]-1-piperazinyl]methyl]-3,4-dihydro-2,5,7,8-tetramethyl-, hydrochloride; 2H-1-benzopyran-6-ol, 2-[[4-[3-(ethylamino)-2-pyridinyl]-1-piperazinyl]methyl]-3,4-dihydro-2,5,7,8-tetramethyl-, (Z)-2-butenedioate; 21-[4-[5,6-bis(diethylamino)-2-pyridinyl]-1-piperazinyl]-16-alpha-methyl-pregna-1,4,9(11)-triene-3,20-dione, hydrochloride; 21-[4-[3-ethylamino)-2-pyridinyl]-1-piperazinyl-16-alpha-methyl-pregna-1,4,9(11)-trien-3,20-dione, -(Z)-2-butenedioate; 21-[4-[3-ethylamino)-2-pyridinyl]-1-piperazinyl-16-alpha-methyl-pregna-1,4,9(11)-trien-3,20-dione, hydrochloride; 21-[4-(2,6-di-1-pyrrolidinyl-4-pyrimidinyl)-1-piperazinyl]-16-alpha-methyl)-pregna-1,4,9(11)-triene-3,20-dione monomethanesulfonate; 21-(4-(2,6-di-1-pyrrolindinyl-4-pyrimidinyl)-1-piperazinyl]-pregna-1,4,9(11)-triene-3,20-dione, (Z)-2-butenedioate; 21-(4-(2,6-di-1-pyrrolindinyl-4-pyrimidinyl)-1-piperazinyl]-pregna-1,4,9(11)-triene-3,20-dione, monomethanesulfonate; 16-alpha-methyl-21-[4-[4,6-bis(2-pyridinyl)-1,3,5-triazin-2-yl]-1-piperazinyl]-pregna-1,4,9(11)-triene-3,20-dione, monomethanesulfonate; or 16-alpha-methyl-21-[4-[2,6-bis(2-pyridinyl)-4-pyrimidinyl)-1-piperazinyl]-pregna-1,4,9(11)-triene-3,20-dione, monomethanesulfonate.
Claim 5
Dependent Claim
17 words
A method according to claim 1, wherein said lazaroid comprises 2-[(2,6-di-1-pyrrolidinyl)-4-pyrimidinyl-methylaminoethanol or 4-[3-(ethylamino)-2-pyridinyl] piperazine and salts thereof.
Claim 6
Dependent Claim
12 words
A method according to claim 1, wherein said tissue repair comprises re-epithelization.
Claim 7
Dependent Claim
13 words
A method according to claim 1, wherein said tissue repair comprises mesothelial repair.
Claim 8
Dependent Claim
31 words
A method according to claim 1, wherein the lazaroid is administered in conjunction with a delivery vehicle which maintains an effective local concentration at the injury site of said lazaroid compound.
Claim 9
Dependent Claim
22 words
A method according to claim 7, wherein said effective local concentration ranges between about 0.007 ng and about 0.033 mg/hr/cm 2 .
Claim 10
Dependent Claim
22 words
A method according to claim 8, wherein said effective local concentration ranges between about 0.007 μg and about 6.7 μg/hr/cm 2 .
Claim 11
Dependent Claim
20 words
A method according to claim 7, wherein said effective local concentration ranges between about 0.04 ng and about 0.2 mg/hr/kg.
Claim 12
Dependent Claim
20 words
A method according to claim 10, wherein said effective local concentration ranges between about 0.04 μg and about 40 μg/hr/kg.
Claim 13
Dependent Claim
19 words
A method according to claim 1, wherein the lazaroid compound is administered in the form of microcapsules or microspheres.
Claim 14
Dependent Claim
34 words
A method according to claim 12, wherein the microcapsules or microspheres comprise a biodegradable polymer selected from the group consisting of poly(dl-lactides), poly(dl-lactide-co-glycolides), polycaprolactones, polyglycolides, polylactic acid-co-glycolides, poly(hydroxybutyric acids), polyortho-esters, polyacetals and mixtures thereof.
Claim 15
Dependent Claim
18 words
A method according to claim 1, wherein the lazaroid compound is administered in a form of a film.
Claim 16
Dependent Claim
32 words
A method according to claim 14, wherein the film comprises a biodegradable polymer selected from the group consisting of poly(dl-lactides), poly(dl-lactide-co-glycolides), polycaprolactones, polyglycolides, polylactic acid-co-glycolides, poly(hydroxybutyric acids), polyortho-esters, polyacetals and mixtures thereof.
Claim 17
Dependent Claim
17 words
A method according to claim 1, wherein the lazaroid compound is administered in the form of liposomes.
Claim 18
Dependent Claim
12 words
A method according to claim 16, wherein the liposomes comprise L-alpha-distearoyl phosphatidylcholine.
Claim 19
Dependent Claim
19 words
A method according to claim 1, wherein the lazaroid compound is administered in the form of a lipid foam.
Claim 20
Dependent Claim
18 words
A method according to claim 1, wherein the lazaroid compound is administered in the form of an instillate.
Claim 21
Dependent Claim
30 words
A method according to claim 19, wherein the instillate comprises a high-molecular-weight carrier selected from the group consisting of dextrans, cyclodextrans, hydrogels, carboxymethylcellulose, hyaluronic acid, chondroitin sulfate and mixtures thereof.
Claim 22
Dependent Claim
19 words
A method according to claim 1, wherein the lazaroid compound is administered in combination with an absorbable mechanical barrier.
Claim 23
Dependent Claim
15 words
A method according to claim 21, wherein the absorbable mechanical barrier comprises oxidized regenerated cellulose.
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