Patent US4853225A successfully refreshed from Google Patents.
← Back to Patent Explorer
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
📄 Original PDF 🌐 Google Patents 🔄 Sync Now

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

Assigned Categories & Tags

No categories assigned to this patent yet.

Assign Category Tag