Patent US4853225A successfully refreshed from Google Patents.
US4853225A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Process for implanting a medicament depot
Assignee: Merck Patent GmbH
•
Filing: 1986-12-05
•
Granted: 1989-08-01
•
Expires: 2006-12-05
Abstract
Abstract The invention relates to an implantable medicament depot comprising physiologically acceptable excipients and at least one delayed release active compound which is a chemotherapeutic of the gyrase inhibitor type. The depot can be used for combating infections.
Inventors
- 👤 Helmut Wahlig
- 👤 Elvira Dingeldein
- 👤 Johannes Rothe
- 👤 Wolfgang Stille
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-24 09:06
CPC Classifications
A; A61; A61K; A61K45/00; A61K45/06; A61K9/00; A61K9/0012; A61K9/0019; A61K9/0024; A61L; A61L24/00; A61L24/001; A61L24/0015; A61L2300/00; A61L2300/40; A61L2300/432; A61L2300/434
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
58 words
A method of combating an infection in a patient in whom the infection already exits, comprising implanting in the patient an implantable medicament depot consisting essentially of a physiologically acceptable excipient which achieves delayed release of an active agent and an infection-treating effective amount of at least one chemotherapeutic gyrase inhibitor as the active agent for delayed release.
Claim 2
Independent Claim
58 words
A method of combating an infection in a patient in whom the infection already exits, comprising implanting in the patient an implantable medicament depot consisting essentially of a physiologically acceptable excipient which achieves delayed release of an active agent and an infection-treating effective amount of at least one chemotherapeutic gyrase inhibitor as the active agent for delayed release.
Claim 3
Dependent Claim
196 words
A method of claim 1, wherein the gyrase inhibitor is a compound of the formula ##STR2## wherein X is N or CR 6 , Y is N or CR 8 , Z is N or CH, R 1 is alkyl, alkenyl, hydroxyalky, Hal-alkyl, NR 9 R 10 , OR 11 , cycloalkyl, Ar or Ar-alkyl, R 3 is H or alkyl, R 5 is H, Hal, alkyl or alkoxy, R 6 is H, Hal, alkyl, alkoxy or NO 2 , R 7 is alkyl, Hal, NR 9 R 10 , a 5- or 6-membered N-containing aromatic or aliphatic heterocycle, such as heterocycle containing an additional hetero O, N or S atom, or either of said heterocycles which is substituted, or R 6 and R 7 together form methylenedioxy, R 8 is H, Hal, alkyl or alkoxy or R 8 and R 1 together form --O--CH 2 --CHalkyl or --CH 2 CH 2 --CHalkyl, R 9 , R 10 and R 11 are each H or alkyl, Ar is phenyl or substituted phenyl, Hal is F, Cl, Br or I, and the alkyl, cycloalkyl, alkenyl and alkoxy groups in each case contain up to 6 C atoms.
Claim 4
Dependent Claim
127 words
A method of claim 2 wherein Y is N or CR 8 , Z is N or CH, R 1 is alkyl, Hal-alkyl, NH-alkyl, O-alkyl, cycloalkyl or Hal-phenyl, R 3 is H, R 5 is H, R 6 is H or Hal, R 7 is alkyl, Hal or a 5- or 6-membered N-containing aromatic or aliphatic heterocycle which optionally can contain a further N atom, each optionally substituted by one or two alkyl, amino or alkylaminoalkyl groups, or R 6 and R 7 together are methylenedioxy, R 8 is H, Hal or alkyl, or R 8 and R 1 together are --O--CH 2 --CHalkyl or --CH 2 CH 2 --CHalkyl and Hal is F or Cl and the alkyl groups in each case contain 1-3 C atoms.
Claim 5
Dependent Claim
107 words
The method of claim 2 wherein Y is N or CR 8 , Z is N or CH, R 1 is alkyl, 2-fluoroethyl, methylamino, methoxy, cyclopropyl or p-fluorophenyl, R 3 and R 5 are each H, R 6 is H or F, R 7 is methyl, Cl, pyrrl, pyrrolidino, 3,4-dimethylpyrrolidino, 3-aminopyrrolidino, 3-amino-4-methylpyrrolidino, 3-ethylaminomethyl-pyrrolidino, pyridyl, piperidyl, piperazino or 3- or 4-methylpiperazino, or R 6 and R 7 together are methylenedioxy and R 8 is H, methyl or F, or R 8 and R 1 together are --OCH 2 --CH(CH 3 )--or --CH 2 CH 2 --CH(CH 3 )--and the alkyl groups in each case contain 1-3 C atoms.
Claim 6
Dependent Claim
61 words
A method of claim 2 wherein Y is N or CR 8 Z is N or CH, R 1 is ethyl or cyclopropyl, R 3 and R 5 are each H, R 6 is F, R 7 is piperazino or 3- or 4-methylpiperazino, and R 8 is H, or R 8 and R 1 together are --O--CH 2 --CH(CH 3 ).
Claim 7
Dependent Claim
54 words
A method of claim 1 wherein the gyrase inhibitor is ciprofloxacin, ofloxacin, amifloxacin, cinoxacin, difloxacin (A-56619), enoxacin, flumequin, irloxacin, miloxacin, malidixic acid, norfloxacin, oxolic acid, pefloxacin, pipemidic acid, piromidic acid, rosoxacin, A-56620, A-57132, A-60969, A-656619, A-656620, AM-833, AT-3295, AT-3765, CI-934, E-3432, E-3499, EN-272, NY-198, OPC-7594, Ro-23-6240, S-25930, S-25932, T-14097, 79286-76-3, 80-107118, or 1-ethyl-2-phenyl-4-pyridone-5-carboxylic acid.
Claim 8
Dependent Claim
15 words
A method of claim 1 wherein the amount of active agent is 0.01 to 10%.
Claim 9
Dependent Claim
9 words
A method of claim 1 which is an implant.
Claim 10
Dependent Claim
15 words
A method of claim 1 wherein said depot is a bone cement or bone filler.
Claim 11
Dependent Claim
14 words
A method of claim 1 wherein the excipient comprises a polyacrylate or a polymethacrylate.
Claim 12
Dependent Claim
11 words
A method of claim 1 wherein the excipient is tricalcium phosphate.
Claim 13
Dependent Claim
10 words
A method of claim 1 wherein the excipient is collagen.
Claim 14
Dependent Claim
13 words
A method of claim 1 wherein the excipient is a polysaccharide or fibrin.
References Cited (Backward Citations)
US3857932A
Cited
US3882858A
Cited
US4191740A
Cited
US4203442A
Cited
US4322398A
Cited
US4291013A
Cited
US4293539A
Cited
GB2093348A
Cited
US4617293A
Cited
US4357312A
Cited
US4563485A
Cited
US4619913A
Cited
US4595713A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-07-31 | 1993-01-30 | 1993-08-01 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-07-31 | 1997-01-30 | 1997-08-01 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-07-31 | 2001-01-30 | 2001-08-01 | $7700.00 | Window Closed / Lapsed |