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US4399145A Expired / Lapsed US ⏱️ 0.0 years remaining

Lactams Compositions and pharmaceutical methods of use

Assignee: Grünenthal GmbH
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Filing: 1981-11-05
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Granted: 1983-08-16
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Expires: 2001-11-05
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Abstract

Abstract The invention relates to new lactam compounds, pharmaceutical compositions containing them (especially those for oral or rectal application) and to processes for the preparation of these compounds and compositions. The new compounds have the general formula ##STR1## wherein X represents a straight or branched alkyl radical with 1 to 4 carbon atoms, preferably a methyl group. The new compounds of formula (I) have sedating-tranquilizing properties. In higher dosages some of them also act as hypno-anesthetics. Moreover the derivative in which X represents the methyl group has anticonvulsant activities. The valuable compounds of formula (I) are prepared in a manner known per se e.g. by reacting an 3-alkyl-3-halogen-2-oxopiperidine (the alkyl having 1-4 carbon atoms) with a metal derivative of 2,3-dihydro-3-oxo-1,2-benzisothiazoldioxid-(1,1) or by reacting an 3-alkyl-3-amino-2-oxopiperidine with o-sulfobenzoic acid dichloride or dibromide or with an o-halomercaptobenzoylhalide, followed by oxydation. Other processes known per se, such as cyclizations to form lactam rings, are also suitable for the preparation of the compounds of formula (I).

Inventors

  • 👤 Ivars Graudums
  • 👤 Elmar Friderichs

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-07 16:26
CPC Classifications
C; C07; C07D; C07D417/00; C07D211/00; C07D211/04; C07D211/68; C07D211/72; C07D211/74; C07D211/76; A; A61; A61P; A61P25/00; A61P25/08; A61P25/20

Claims Analysis

Total Claims: 18
Claim 1
Independent Claim 22 words
A compound of the formula I ##STR11## wherein X represents a straight or branched alkyl radical with 1 to 4 carbon atoms.
Claim 2
Dependent Claim 22 words
A compound of the formula I ##STR11## wherein X represents a straight or branched alkyl radical with 1 to 4 carbon atoms.
Claim 3
Dependent Claim 17 words
The compound of claim 1 wherein X is an alkyl radical with one or two carbon atoms.
Claim 4
Dependent Claim 12 words
The compound of claim 1 which is 3-(2,3-dihydro-1,1-dioxido-3-oxo-1,2-benzisothiazol-2-yl)-3-methyl-2-oxopiperidine having the formula ##STR12##
Claim 5
Dependent Claim 17 words
The compound of claims 1, 2 or 3 which comprise the optically active form of said compound.
Claim 6
Dependent Claim 29 words
A pharmaceutical sedating-tranquilizing, hypno-anesthetic and anticonvulsant composition comprising a biologically acceptable carrier and a therapeutically effective amount of a compound of any one of claims 1, 2, or 3.
Claim 7
Dependent Claim 15 words
The composition of claim 5 wherein the compound is present in an optically active form.
Claim 8
Dependent Claim 25 words
The composition of claim 5 wherein the compound is present in an amount of from about 50 to about 500 mg per single dosage form.
Claim 9
Dependent Claim 18 words
The composition of claims 5 or 6 wherein the composition is in a suitable form for oral administration.
Claim 10
Dependent Claim 19 words
The composition of claim 8 wherein the composition is in a form for retarded release of the active ingredients.
Claim 11
Dependent Claim 15 words
An anticonvulsant composition comprising a biologically acceptable carrier and an effective anticonvulsant amount of 3-(2,3-dihydro-1,1-dioxido-3-oxo-1,2-benzisothiazol-2-yl)-3-methyl-2-oxopiperidine.
Claim 12
Dependent Claim 15 words
An anticonvulsant composition comprising a biologically acceptable carrier and an effective anticonvulsant amount of 3-(2,3-dihydro-1,1-dioxido-3-oxo-1,2-benzisothiazol-2-yl)-3-methyl-2-oxopiperidine.
Claim 13
Dependent Claim 15 words
A hypno-anesthetic composition comprising a biologically acceptable carrier and an effective hypo-anesthetic amount of 3-(2,3-dihydro-3-oxo-1,2-benzisothiazol-2-yl)-3-methyl-2-oxopiperidine.
Claim 14
Dependent Claim 15 words
A hypno-anesthetic composition comprising a biologically acceptable carrier and an effective hypo-anesthetic amount of 3-(2,3-dihydro-3-oxo-1,2-benzisothiazol-2-yl)-3-methyl-2-oxopiperidine.
Claim 15
Independent Claim 35 words
A method of treating a patient suffering from epilepsy which comprises administering to said patient an effective amount of a composition comprising a biologically acceptable carrier and a compound of claims 1, 2 or 3.
Claim 16
Dependent Claim 27 words
A method of therapeutically or prophylactically treating a patient for convulsions which comprises administering to said patient an effective amount of a composition according to claim 10.
Claim 17
Independent Claim 36 words
A method of sedating a patient in need of sedation comprising administering to said patient an effective amount of a composition comprising a suitable biologically acceptable carrier and a compound of claims 1, 2 or 3.
Claim 18
Dependent Claim 11 words
The method of claim 14 wherein the composition is administered orally.

References Cited (Backward Citations)

US3951985A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1986-08-15 1987-02-14 1987-08-16 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1990-08-15 1991-02-14 1991-08-16 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1994-08-15 1995-02-14 1995-08-16 $7700.00 Window Closed / Lapsed

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