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US4442084A Expired / Lapsed US ⏱️ 0.0 years remaining

Analgesic and myotonolytic preparations

Assignee: Sandoz AG
•
Filing: 1982-08-11
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Granted: 1984-04-10
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Expires: 2002-08-11
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Abstract

Abstract Compositions having enhanced analgesic and myotonolytic activity comprising as active agents (a) an analeptically active quinazolinone and (b) a centrally acting myotonolytic.

Inventors

  • 👤 Dietmar Romer

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-27 18:50
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/495; A61K31/505

Claims Analysis

Total Claims: 20
Claim 1
Independent Claim 86 words
A pharmaceutical preparation in oral form useful in inducing analgesia and/or in treating myotonolytic conditions comprising: as active agent (a), an analgesically active quinazoline compound selected from the group consisting of 1-isopropyl-4-(4-fluorophenyl)-6,7-methylenedioxy-2(1H)-quinazolinone; 1-isopropyl-4-phenyl-7-methyl-2(1H)-quinazolinone; 1-isopropyl-4-phenyl-6,7-methylenedioxy-2(1H)-quinazolinone; 1-isopropyl-4-(4-fluorophenyl)-7-methyl-2-(1H)-quinazolinone; 1-cyclopropylmethyl-4-phenyl-6-methoxy-2(1H)-quinazolinone; and 1-(2,2,2-trifluoroethyl)-4-phenyl-6-chloro-2(1H)-quinazolinone, and as active agent (b), a centrally acting myotonolytic compound selected from 5-chloro-7-methyl-4-(-imidazolin-2-ylamino)-2,1,3-benzothiadiazole and 5-chloro-4-(2-imidazolin-2-ylamino)-2,1,3-benzothiadiazole, said active agents (a) and (b) being present in the pharmaceutical preparation in a ratio of active agent (a) to active agent (b) of from about 5:1 to about 100:1 parts by weight.
Claim 2
Dependent Claim 86 words
A pharmaceutical preparation in oral form useful in inducing analgesia and/or in treating myotonolytic conditions comprising: as active agent (a), an analgesically active quinazoline compound selected from the group consisting of 1-isopropyl-4-(4-fluorophenyl)-6,7-methylenedioxy-2(1H)-quinazolinone; 1-isopropyl-4-phenyl-7-methyl-2(1H)-quinazolinone; 1-isopropyl-4-phenyl-6,7-methylenedioxy-2(1H)-quinazolinone; 1-isopropyl-4-(4-fluorophenyl)-7-methyl-2-(1H)-quinazolinone; 1-cyclopropylmethyl-4-phenyl-6-methoxy-2(1H)-quinazolinone; and 1-(2,2,2-trifluoroethyl)-4-phenyl-6-chloro-2(1H)-quinazolinone, and as active agent (b), a centrally acting myotonolytic compound selected from 5-chloro-7-methyl-4-(-imidazolin-2-ylamino)-2,1,3-benzothiadiazole and 5-chloro-4-(2-imidazolin-2-ylamino)-2,1,3-benzothiadiazole, said active agents (a) and (b) being present in the pharmaceutical preparation in a ratio of active agent (a) to active agent (b) of from about 5:1 to about 100:1 parts by weight.
Claim 3
Dependent Claim 12 words
A preparation according to claim 1, wherein active agent (a) is 1-isopropyl-4-(4-fluorophenyl)-7-methyl-2(1H)-quinazolinone.
Claim 4
Dependent Claim 12 words
A preparation according to claim 1 wherein active agent (a) is 1-isopropyl-4-phenyl-7-methyl-2(1H)-quinazolinone.
Claim 5
Dependent Claim 12 words
A preparation according to claim 1 wherein active agent (b) is 5-chloro-4-(2-imidazolin-2-ylamino)-2,1,3-benzothiadiazole.
Claim 6
Dependent Claim 18 words
A preparation according to claim 1 wherein active agent (a) is 1-isopropyl-4-(4-fluorophenyl)-7-methyl-2(1H)-quinazolinone and active agent (b) is 5-chloro-4-(2-imidazolin-2-ylamino)-2,1,3-benzothiadiazole.
Claim 7
Dependent Claim 27 words
A preparation according to claim 1, wherein the ratio of active agent (a) to active agent (b) is from about 10:1 to about 50:1 parts by weight.
Claim 8
Dependent Claim 19 words
A preparation according to claim 6 wherein the ratio is from about 25:1 to about 50:1 parts by weight.
Claim 9
Dependent Claim 15 words
A preparation according to claim 7 wherein the ratio is about 25:1 parts by weight.
Claim 10
Dependent Claim 10 words
A preparation according to claim 1, in unit dosage form.
Claim 11
Dependent Claim 17 words
A preparation according to claim 9 containing from about 25 to 50 mg of active agent (a).
Claim 12
Dependent Claim 19 words
A pharmaceutical preparation according to claim 1 wherein active agent (a) is 1-isopropyl-4-phenyl-7-methyl-2(1H)-quinazolinone and active agent (b) is 5-chloro-4-(2-imidazolin-2-ylamino)-2,1,3-benzothiadiazole.
Claim 13
Dependent Claim 32 words
A method of inducing analgesia and/or of treating myotonolytic conditions comprising orally administering to a subject in need of such treatment a therapeutically effective amount of a pharmaceutical preparation of claim 1.
Claim 14
Dependent Claim 12 words
A method according to claim 12 wherein active agent (a) is 1-isopropyl-4-(4-fluorophenyl)-7-methyl-2(1H)-quinazolin-one.
Claim 15
Dependent Claim 12 words
A method according to claim 12 wherein active agent (b) is 5-chloro-4-(2-imidazolin-2-ylamino)-2,1,3-benzothiadiazole.
Claim 16
Dependent Claim 25 words
A method according to claim 12 wherein the ratio of active agent (a) to (b) is from about 25:1 to about 50:1 parts by weight.
Claim 17
Dependent Claim 21 words
A method according to claim 12 wherein the daily dosage of active agent (a) administered is from 25 to 600 mg.
Claim 18
Dependent Claim 12 words
A method according to claim 12 wherein active agent (a) is 1-isopropyl-4-phenyl-7-methyl-2(1H)-quinazolinone.
Claim 19
Dependent Claim 18 words
A method according to claim 17 wherein active agent (a) is 1-isopropyl-4-(4-fluorophenyl)-7-methyl-2(1H)-quinazolinone and active agent (b) is 5-chloro-4-(2-imidazolin-2-ylamino)-2,1,3-benzothiadiazole.
Claim 20
Dependent Claim 18 words
A method according to claim 11 wherein active agent (a) is 1-isopropyl-4-phenyl-7-methyl-2(1H)-quinazolinone and active agent (b) is 5-chloro-4-(2-imidazolin-2-ylamino)-2,1,3-benzothiadiazole.

References Cited (Backward Citations)

GB1248430A Cited
GB1379677A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1987-04-10 1987-10-10 1988-04-10 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1991-04-10 1991-10-10 1992-04-10 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1995-04-10 1995-10-10 1996-04-10 $7700.00 Window Closed / Lapsed

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