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Anesthetic polyorganophosphazenes

Assignee: Research Corp
•
Filing: 1982-06-21
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Granted: 1985-01-22
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Expires: 2002-06-21
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Abstract

Abstract A long-acting, local anesthetic, comprising a polymeric phosphazene backbone, and 2-amino-4-picoline radical having local anesthetic activity and an amino functional group on the ring of said radical through which said radical is covalently attached to the phosphazene backbone by a phosphorous-nitrogen single bond is disclosed along with medicaments containing such anesthetics.

Inventors

  • 👤 Harry R. Allcock
  • 👤 Paul E. Austin
  • 👤 Thomas X. Neenan

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-23 18:10
CPC Classifications
C; C08; C08G; C08G79/00; C08G79/02; C08G79/025; A; A61; A61K; A61K31/00; A61K31/74; A61K31/80; A61K47/00; A61K47/50; A61K47/51; A61K47/56; A61K47/59; A61K47/605

Claims Analysis

Total Claims: 22
Claim 1
Independent Claim 69 words
A long-acting, local anesthetic, comprising: a polymeric phosphazene backbone, and an organic radical having local anesthetic activity and an amino functional group on a phenyl ring through which said radical is covalently attached to said phosphazene backbone by a phosphorous-nitrogen single bond, and said organic radical being selected from the group consisting of radicals of benzocaine, butethamine, butyl ester of p-aminobenzoic acid, m-butethamine, procaine, chloroprocaine proparacaine, propoxycaine and tetracaine.
Claim 2
Dependent Claim 69 words
A long-acting, local anesthetic, comprising: a polymeric phosphazene backbone, and an organic radical having local anesthetic activity and an amino functional group on a phenyl ring through which said radical is covalently attached to said phosphazene backbone by a phosphorous-nitrogen single bond, and said organic radical being selected from the group consisting of radicals of benzocaine, butethamine, butyl ester of p-aminobenzoic acid, m-butethamine, procaine, chloroprocaine proparacaine, propoxycaine and tetracaine.
Claim 3
Dependent Claim 15 words
The local anesthetic of claim 1, wherein said organic radical is a radical of benzocaine.
Claim 4
Dependent Claim 15 words
The local anesthetic of claim 1, wherein said organic radical is a radical of butethamine.
Claim 5
Dependent Claim 15 words
The local anesthetic of claim 1, wherein said organic radical is a radical butyl 4-aminobenzoate.
Claim 6
Dependent Claim 15 words
The local anesthetic of claim 1, wherein said organic radical is a radical of procaine.
Claim 7
Dependent Claim 15 words
The local anesthetic of claim 1, wherein said organic radical is a radical of tetracaine.
Claim 8
Dependent Claim 15 words
The local anesthetic of claim 1, wherein said organic radical is a radical of propoxycaine.
Claim 9
Dependent Claim 15 words
The local anesthetic of claim 1, wherein said organic radical is a radical of proparacaine.
Claim 10
Dependent Claim 15 words
The local anesthetic of claim 1, wherein said organic radical is a radical of chloroprocaine.
Claim 11
Dependent Claim 15 words
The local anesthetic of claim 1, wherein said polymeric phosphazene backbone is a cyclic trimer.
Claim 12
Dependent Claim 23 words
The local anesthetic of claim 1, wherein said polymeric phosphazene backbone is a linear chain containing from 3 to 30,000 ##STR16## repeating units.
Claim 13
Dependent Claim 16 words
The local anesthetic of claim 11, wherein said backbone contains from 100 to 20,000 repeating units.
Claim 14
Dependent Claim 14 words
The local anesthetic of claim 11, wherein said backbone contains about 15,000 repeating units.
Claim 15
Dependent Claim 49 words
A long-acting, local anesthetic, comprising: a polymeric phosphazene backbone, and an organic radical having local anesthetic activity which is an ester of p-aminobenzoic acid and an amino functional group on a phenyl ring through which said radical is covalently attached to said phosphazene backbone by a phosphorous-nitrogen single bond.
Claim 16
Dependent Claim 49 words
A long-acting, local anesthetic, comprising: a polymeric phosphazene backbone, and an organic radical having local anesthetic activity which is an ester of p-aminobenzoic acid and an amino functional group on a phenyl ring through which said radical is covalently attached to said phosphazene backbone by a phosphorous-nitrogen single bond.
Claim 17
Dependent Claim 21 words
The local anesthetic of claim 14, wherein a position on a phenyl ring ortho to said amino functional group is unsubstituted.
Claim 18
Dependent Claim 15 words
The local anesthetic of claim 15, wherein said polymeric phosphazene backbone is a cyclic trimer.
Claim 19
Dependent Claim 22 words
The local anesthetic of claim 15, wherein said polymeric phosphazene backbone is a linear chain containing from 100 to 20,000 repeating units.
Claim 20
Dependent Claim 14 words
The local anesthetic of claim 1, wherein said backbone contains about 15,000 repeating units.
Claim 21
Dependent Claim 24 words
A long-acting local anesthetic medicament, comprising a local anesthetic effective amount of a compound of claim 1 in admixture with a pharmaceutically acceptable carrier.
Claim 22
Dependent Claim 18 words
A long-acting local anesthetic medicament, comprising a compound of claim 1 in admixture with a pharmaceutically acceptable carrier.

References Cited (Backward Citations)

US4055523A Cited
US4130547A Cited
US4207403A Cited
US4221904A Cited
US4242491A Cited
US4218557A Cited
US4223102A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1988-01-22 1988-07-23 1989-01-22 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1992-01-22 1992-07-23 1993-01-22 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1996-01-22 1996-07-23 1997-01-22 $7700.00 Window Closed / Lapsed

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