摘要:
Composés de quinolonyle lactames anti-microbiens comprenant une fraction lactame liée à une fraction quinolone de la formule (I), dans laquelle (1) A1, A2, A3, R1 et R4 forment n'importe quelle fraction d'une variété de fractions quinolone, naphtyridine ou cycliques apparentées connues dans le domaine pour présenter une activité anti-microbienne.; et (2) R6 représente une partie d'une fraction de liaison, reliant la fraction quinolone à une fraction lactame ayant la formule (II), dans laquelle (3) 10, R11, R12, R13 et R14 forment avec les liaisons ''a'' et ''b'' n'importe quelle fraction d'une variété de fractions lactames connues dans le domaine pour présenter une activité anti-microbienne; et (4) la fraction de liaison comprend (par exemple) des groupes carbamate, dithiocarbamate, urée, thiourée, isouronium, isothiouronium, guanidine, carbonate, trithiocarbonate, carbamate inversé, xanthate, isouronium inversé, dithiocarbamate, isothiouronium inversé, amine, imine, ammonium, hétéroarylium, éther, thioéther, ester, thioester, amide, et hydrazide.
摘要:
Antimicrobial lactam-quinolone compounds comprising a lactam-containing moiety linked to a quinolone moiety, of the formula: wherein ( 1 ) A', A 2 , A3, R 1 , R 4 and R 6 generally form any of a variety of quinolone, naphthyridine or related cyclic moieties known in the art to have animicrobial activity; and (2) R' or R 3 contain a linking moiety, linking the quinolone moiety to a lactam-containing moiety having the formula: wherein (3) R 10 , R 11 , R 12 , R 13 , and R 14 , together with bonds "a" and "b", form any of a variety of lactam-containing moieties known in the art to have antimicrobial activity; and (4) the linking moiety includes (for example) carbamate, dithiocarbamate, urea, thiourea, isouronium, isothiouronium, guanidine, carbonate, trithiocarbonate, reversed carbamate, xanthate, reversed isouronium, reversed dithiocarbamate, reversed isothiouronium, amine, imine, ammonium, heteroarylium, ether, thioether, phosphone, phosphoramide, phosphate, sulfonamide, ester, thioester, amide, and hydrazide groups.
摘要:
Antimicrobial quinolonyl lactam esters comprising a lactam-containing moiety linked, by an ester group, to the 3-carboxy group of a quinolone moiety. These compounds are of the formula: wherein (1) R 3 , R 4 , and R 5 , together with bonds "a" and "b", form certain lactam-containing moieties similar to those known in the art to have antimicrobial activity; and (2) A, R 6 , R 7 , and R 8 form any of a variety of quinolone or napthyridine structures similar to those known in the art to have antimicrobial activity.
摘要:
A medicament package for improving compliance with a therapeutic regimen. The therapeutic regimen involves a plurality of medications administered to a patient in a prescribed sequence and in accordance with specified intervals. The package includes a multiplicity of blister cards (50) of generally uniform planar dimensions. The blister cards (50) carrying the medicaments in sequential order on the individual cards and from card to card. The blister cards (50) being placed in stacked array with the principal dimensions thereof oriented generally horizontally and arranged in order of use with the first to be used topmost. Also included is a base which houses the stack of blister cards and is adapted to support the stack vertically and provides lateral support to the edges of the blister cards. The base permits direct and unobstructed access to the uppermost blister card and limited access only to the edges of the blister cards (50). A lid (22) is adapted to cover the base and movable to an open position allowing access to the uppermost blister card. Each blister card (50) generally contains indicia denoting the order and sequence when the contents of a particular blister cavity are to be consumed.
摘要:
Nitrofurantoin particulates comprising discrete particulates of nitrofurantoin wherein:
(a) said particulates are larger than about 200 mesh size; and (b) the BET surface area of said particulates is at least about 0.2 M²/g. Preferably, the surface of said particulates consists essentially of nitrofurantoin monohydrate. Also preferably, said particulates comprise at least about 5%, more preferably at least about 50% of nitrofurantoin monohydrate. Preferred compositions of this invention comprise these nitrofurantoin particulates in an aqueous suspension. The nitrofurantoin particulates of this invention are highly efficacious for the delivery of nitrofurantoin in oral dosage forms.
摘要:
A method of preventing epileptic seizures in a human or lower animal subject susceptible to said seizures, comprising systemically administering to said subject a safe and effective amount of a compound of the formula: wherein
(a) X is halo or nil, and Y is a substituent selected from the group consisting of unsubstituted or halogen-substituted methyl, halo, nitro, amino, and methoxy; and (b) R is N(R³)₂, OR¹N(R³)₂, N(R²)R¹N(R³)₂, or N(R²)N(R³)₂; where R¹ is C₁-C₃ alkyl which is unsubstituted or substituted with C₁-C₂ alkyl; R² is hydrogen or lower alkyl; and each R³ is, independently, hydrogen or lower alkyl, or both R³ groups are connected to form a saturated 5- or 6-membered heterocycle containing 1 or 2 heteroatoms selected from oxygen and nitrogen and said heterocycle is unsubstituted or substituted with lower alkyl or hydroxy-substituted lower alkyl; or a pharmaceutically-acceptable salt thereof. Preferably X is halo, preferably Y is trifluoromethyl, and R is preferably 3-diethylamino-2,2-dimethylpropoxy.
摘要:
A child resistant box (20) which is composed of a base (23), a lid (22) and a hinge (30) connecting the base (23) and lid (22) together. A latching mechanism is located on each of the two sides of the box for releasably retaining the lid (22) to the base (23). The box (20) can be moved between open, intermediate, and closed positions. The box (20) also includes a means for biasing the lid from the intermediate position toward the closed position. To open the box (20) the lid (22) is compressed to the intermediate position. In this intermediate position, the latching mechanism may be disengaged by exerting manual pressure thereon toward the center of the box (20). Once pressure is exerted simultaneously on both latching mechanisms the lid (22) is released and the biasing means moves the lid (22) at least partially toward the open position. The operation of this box (20) is particularly well-suited for the elderly. Although this child resistant box can house virtually anything, it is particularly well suited for housing a set of blister cards which include a plurality of medicaments to be taken at different times during a therapeutic regimen.
摘要:
The present invention involves certain N-hydroxy-5-phenyl-2-furancarboximidamides, pharmaceutical compositions containing such compounds, and methods for increasing the contractile force of cardiac muscle of a mammal which comprises systemically administering such compounds to a mammal.
摘要:
The invention involves a sustained release pharmaceutical capsule for oral administration comprising, in a capsule shell, a particulate mixture comprising an active drug ingredient which is a weak acid, neutral, or a weak base, polyvinylpyrrolidone, and carboxyvinylpolymer.