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US4147804A
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Amidinourea local anesthetics
Assignee: William H Rorer Inc
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Filing: 1977-05-25
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Granted: 1979-04-03
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Expires: 1997-05-25
Abstract
Abstract A method for producing local anesthetic action in a patient by administering amidinoureas.
Inventors
- 👤 Julius Diamond
- 👤 George H. Douglas
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 08:09
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/16; A61K31/17; A61K31/33
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
108 words
A method for producing local anesthetic action in a patient which comprises administering parenterally to said patient an effective daily dosage of between 0.1 and 70 mg/kg of body weight of said patient a compound of the formula: ##STR11## where: R 2 , R 3 , R 4 , R 5 and R 6 may be the same or different and are: hydrogen, halo, loweralkyl, haloloweralkyl, nitro, amino, acylamino or loweralkoxy; R n is hydrogen or loweralkyl; and R 7 , r 8 , r 9 and R 10 are: hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkylloweralkyl, alkoxyloweralkyl, aralkoxyloweralkyl or aralkyl; and the non-toxic acid addition salts thereof.
Claim 2
Independent Claim
108 words
A method for producing local anesthetic action in a patient which comprises administering parenterally to said patient an effective daily dosage of between 0.1 and 70 mg/kg of body weight of said patient a compound of the formula: ##STR11## where: R 2 , R 3 , R 4 , R 5 and R 6 may be the same or different and are: hydrogen, halo, loweralkyl, haloloweralkyl, nitro, amino, acylamino or loweralkoxy; R n is hydrogen or loweralkyl; and R 7 , r 8 , r 9 and R 10 are: hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkylloweralkyl, alkoxyloweralkyl, aralkoxyloweralkyl or aralkyl; and the non-toxic acid addition salts thereof.
Claim 3
Dependent Claim
99 words
The method of claim 1 where: R 2 is hydrogen, methyl or ethyl; R 3 and R 5 are hydrogen; R 4 is hydrogen, methyl, ethyl, chloro or bromo; R 6 is hydrogen, methyl, ethyl, nitro, methoxy, ethoxy, chloro, bromo or fluoro; R n is hydrogen, methyl or ethyl, and R 7 , r 8 , r 9 and R 10 are hydrogen, methyl, ethyl, propyl, i-propyl, butyl, i-butyl, sec-butyl, t-butyl, pentyl, hexyl, heptyl, allyl, propargyl, methoxyethyl, ethoxyethyl, benzyloxyethyl; provided R 7 , R 8 , R 9 and R 10 are not all hydrogen at the same time.
Claim 4
Dependent Claim
40 words
The method of claim 2 where: R 2 and R 6 are diloweralkyl; R n , R 3 , R 4 , R 5 , R 8 , R 9 and R 10 are hydrogen and R 7 is loweralkyl.
Claim 5
Dependent Claim
16 words
The method of claim 3 where: R 2 , r 6 and R 7 are methyl.
Claim 6
Dependent Claim
18 words
The method of claim 3 where: R 2 and R 6 are ethyl and R 7 is methyl.
Claim 7
Independent Claim
105 words
A method for producing local anesthetic action in a patient which comprises administering topically to said patient a composition containing, in the range of 0.1-10% by weight of said composition, a compound of the formula: ##STR12## where: R 2 , R 3 , R 4 , R 5 and R 6 may be the same or different and are: hydrogen, halo, loweralkyl, haloloweralkyl, nitro, amino, acylamino or loweralkoxy R n is hydrogen or loweralkyl; and R 7 , r 8 , r 9 and R 10 are: hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkylloweralkyl, alkoxyloweralkyl, aralkoxyloweralkyl or aralkyl; and the non-toxic acid addition salts thereof.
Claim 8
Independent Claim
105 words
A method for producing local anesthetic action in a patient which comprises administering topically to said patient a composition containing, in the range of 0.1-10% by weight of said composition, a compound of the formula: ##STR12## where: R 2 , R 3 , R 4 , R 5 and R 6 may be the same or different and are: hydrogen, halo, loweralkyl, haloloweralkyl, nitro, amino, acylamino or loweralkoxy R n is hydrogen or loweralkyl; and R 7 , r 8 , r 9 and R 10 are: hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkylloweralkyl, alkoxyloweralkyl, aralkoxyloweralkyl or aralkyl; and the non-toxic acid addition salts thereof.
Claim 9
Dependent Claim
100 words
The method of claim 6 where: R 2 is hydrogen, methyl or ethyl; R 3 and R 5 are hydrogen; R 4 is hydrogen, methyl, ethyl, chloro or bromo; R 6 is hydrogen; methyl, ethyl, nitro, methoxy, ethoxy, chloro, bromo or fluoro; R n is hydrogen, methyl or ethyl, and R 7 , r 8 , r 9 and R 10 are hydrogen methyl, ethyl, propyl, i-propyl, butyl, i-butyl, sec-butyl, t-butyl, pentyl, hexyl, heptyl, allyl, propargyl, methoxyethyl, ethoxyethyl, or benzyloxyethyl; provided R 7 , R 8 , R 9 and R 10 are not all hydrogen at the same time.
Claim 10
Dependent Claim
40 words
The method of claim 7 where: R 2 and R 6 are diloweralkyl; R n , R 3 , R 4 , R 5 , R 8 , R 9 and R 10 are hydrogen and R 7 is loweralkyl.
Claim 11
Dependent Claim
16 words
The method of claim 8 where: R 2 , r 6 and R 7 are methyl.
Claim 12
Dependent Claim
18 words
The method of claim 8 where: R 2 and R 6 are ethyl and R 7 is methyl.
References Cited (Backward Citations)
US3761597A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-04-02 | 1982-10-02 | 1983-04-03 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-04-02 | 1986-10-02 | 1987-04-03 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-04-02 | 1990-10-02 | 1991-04-03 | $7700.00 | Window Closed / Lapsed |