Abstract: Disclosed is a compound selected from the group consisting of 1,3,8-triethyl-2,6-dithioxanthine; 1,3,8-triethyl-2-thioxanthine; 8-cyclopropyl-1-ethyl-3-(2-methyl-butyl)-6-thioxanthine; 1,3-diethyl-8-isopropyl-6-thioxanthine; 8-cyclopropyl-1,3-dipropyl-6-thioxanthine; 8-isopropyl-1,3-dipropyl-6-thioxanthine; 1,3-diethyl-8-cyclopropyl-2,6-dithioxanthine; 1-(4-chlorobenzyl)-3-ethyl-8-isopropyl-6-thioxanthine; and 8-cyclopropyl-1,3-diethyl-6-thioxanthine. Also disclosed is a pharmaceutical composition comprising at least one pharmaceutically acceptable carrier and a compound selected from the group above. Also disclosed is a method of effecting PDE IV inhibition which comprises administering to a patient suffering from a disease or disorder selected from the group consisting of asthma, allergies, PDE IV modulated inflammation, and depression, a therapeutically effective amount of a compound selected from the group above.

Abstract: A method for substantially reducing the range in daily dosages required to control pain in approximately 90% of patients is disclosed whereby an oral solid controlled release dosage formulation having from about 10 to about 40 mg of oxycodone or a salt thereof is administered to a patient. The formulation provides a mean maximum plasma concentration of oxycodone from about 6 to about 60 ng/ml from a mean of about 2 to about 4.5 hours after administration, and a mean minimum plasma concentration from about 3 to about 30 ng/ml from about 10 to about 14 hours after repeated “q12h” (i.e., every 12 hour) administration through steady-state conditions.

Abstract: Bioavailable sustained release oral opioid analgesic dosage forms, comprising a plurality of multiparticulates produced via melt extrusion techniques disclosed.

Abstract: With the above and other objects in view, the present invention comprises compounds having the general formula (I): wherein: R1 is a C2-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, C3-8 cycloalkenyl or cycloalkynyl, wherein said alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl or cycloalkynyl is optionally substituted with hydroxy, C1-5 alkoxy, C3-5 cycloalkoxy, halogen, oxo, carbamido, hydroxycarbamido, oximido, C1-5 alkyloximido, C3-5 cycloalkyloximido, C1-5 acyloximido or C3-5 cycloacyloximido; Q is methylene or ethylene; R3 is aryl or heteroaryl wherein said aryl or heteroaryl has one to three substituents selected from the group consisting of C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C3-6 cycloalkenyl, cycloalkynyl, C3-5 alkylene, C3-5 cycloalkylene, haloC1-6 alkyl, haloC1-6 cycloalkyl, hydroxy, C1-5 alkoxy, C3-5 cycloalkoxy, C1-2 alkylenedioxy, C1-6 acyl, C3-6 cycloacyl, C1-6 acyloxy, C3-6 cycloacyloxy, halogen, nitro or cyano; R8 is C1-5 alkyl or C3-5 cycl

Abstract: Sustained release local anesthetic formulations are administered intra articularly and/or into body spaces/cavities. The formulation is preferably a plurality of injectable microparticles including a local anesthetic and an effective amount of a biocompatible, biodegradable, sustained release material prolonging the release of the local anesthetic and optionally and a pharmaceutically acceptable, i.e., non-toxic, augmenting agent effective to prolong the duration of the local anesthesia for a time period longer than that obtainable without the augmenting agent.

Abstract: Novel compounds which are effective PDE IV inhibitors are disclosed. These compounds have the general structure of: where R1, R2, R3, R4, X1, X2 and Z are described herein. The compounds possess improved PDE IV inhibition as compared to rolipram as well as with improved selectivity with regard to PDE III inhibition. Pharmaceutical compositions containing the same and methods of treatment are also disclosed.

Abstract: Disclosed are compounds of the formula (I): wherein R3 is selected from the group consisting of C1-10 alkyl, C1-10 alkenyl, C3-10 cycloalkyl, C4-10 cycloalkylalkyl or C3-10 cycloalkenyl, wherein said alkyl, alkenyl, cycloalkyl, cycloalkylalkyl or cycloalkenyl is optionally substituted in one position with hydroxy; or benzyl, wherein said benzyl is optionally substituted in one or two positions with halogen, alkoxy, cycloalkoxy or polycycloalkyl, and wherein said alkyl moiety of said alkoxy or cycloalkoxy substituent is optionally substituted in one position with hydroxy; R8 is selected from the group consisting of hydrogen, C1-10 alkyl, C1-10 alkenyl, C3-10 cycloalkyl, C4-10 cycloalkylalkyl or C3-10 cycloalkenyl, wherein said alkyl, alkenyl, cycloalkyl, cycloalkylalkyl or cycloalkenyl is optionally substituted in one position with hydroxy; or benzyl, wherein said benzyl is optionally substituted in one or two positions with halogen, alkoxy, cycloalkoxy or polycycloalkyl, and wherein said a

Abstract: The present invention comprises compounds having the general formula I: wherein: Y, is N or CH Z is selected from the group consisting of alkyl groups such as alkylene groups such as CH2, CH2CH2, CH(CH3); alkenyl groups such as CH═CH; alkynyl groups such as C≡C; and NH, N(C1-C3 alkyl), O, S, C(O)CH2 and OCH2; R1 and R2 are selected from the group consisting of hydrogen and a C1-C8 straight or branched alkyl or a C3-C8 cycloalkyl; R3 is a C3-C12 straight or branched alkyl; R4 is a C3-C10 cycloalkyl optionally substituted with OH or C3-C10 cycloalkenyl optionally substituted with OH; and R8 is a C1-C8 straight or branched alkyl or a C3-C8 cycloalkyl, optionally substituted with OH; and methods of synthesis.

Abstract: A controlled release tablet for oral administration is disclosed which has a tablet core including an insoluble therapeutically active agent having an aqueous solubility of less than or equal to about 5 mg/ml in a sufficient amount to render a therapeutic effect. The core provides rapid release of said therapeutically active agent upon exposure to aqueous solutions. The tablet core is coated with a controlled release coating permitting sustained release of said therapeutically active agent when said coated tablet is exposed to aqueous solutions.

Abstract: Novel compounds which are effective PDE IV inhibitors are disclosed. The present invention is directed to compounds having the general formula I ##STR1## wherein: X is a halogen;Q is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --, a single or a double bond, or --NR.sub.1 --;R.sub.1 is a C.sub.

Abstract: Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds possess improved PDE IV inhibition as compared to theophylline or rolipram as well as with improved selectivity with regard to PDE III inhibition. In certain aspects of the invention, the compounds also demonstrate PDE V inhibition. Pharmaceutical compositions containing the same and methods of treatment are also disclosed.

Abstract: A stable solid controlled release formulation having a coating derived from an aqueous dispersion of a hydrophobic acrylic polymer includes a substrate including an active agent selected from the group consisting of a systemically active therapeutic agent, a locally active therapeutic agent, a disinfecting and sanitizing agent, a cleansing agent, a fragrance agent and a fertilizing agent, overcoated with an aqueous dispersion of the plasticized water-insoluble acrylic polymer. The formulation provides a stable dissolution of the active agent which is unchanged after exposure to accelerated storage conditions.

Abstract: A stabilized solid controlled release dosage form having a coating derived from an aqueous dispersion of ethylcellulose is obtained by overcoating a substrate including a therapeutically active with an aqueous dispersion of ethylcellulose and then curing the coated substrate at a temperature and relative humidity elevated to a suitable level above ambient conditions until the coated dosage form attains a stabilized dissolution profile substantially unaffected by exposure to storage conditions of elevated temperature and/or elevated relative humidity.

Abstract: Novel compounds which are effective PDE IV inhibitors are disclosed. These compounds have the general structure of: ##STR1## where R.sub.1, R.sub.2, R.sub.3, R.sub.4, X.sub.1, X.sub.2 and Z are described herein. The compounds possess improved PDE IV inhibition as compared to rolipram as well as with improved selectivity with regard to PDE III inhibition. Pharmaceutical compositions containing the same and methods of treatment are also disclosed.

Abstract: Solid controlled-release oral dosage forms comprising a therapeutically effective amount of an opioid analgesic or a salt thereof which provide an extended duration of pain relief of about 24 hours, have a dissolution rate in-vitro of the dosage form, when measured by the USP Paddle Method of 100 rpm in 900 ml aqueous buffer at 37.degree. C. from about 12.5% to about 42.5% (by weight) active agent released after 1 hour, from about 25% to about 55% (by weight) active agent released after 2 hours, from about 45% to about 75% (by weight) opioid analgesic released after 4 hours and greater than about 60% (by weight) opioid analgesic released after a hours, the in-vitro release rate being substantially independent of pH and chosen such that the peak plasma level of active agent obtained in-vivo between about 2 and about 8 hours after administration of the dosage form.

Abstract: Disclosed are compounds having the formulae: ##STR1## wherein: Q.sub.3,Q.sub.6a,Q.sub.6b and Q.sub.8 are independently a bond, C.sub.1-8 alkylene, C.sub.2-8 alkenylene and C.sub.2-6 alkynylene, andR.sub.3, R.sub.6a, R.sub.6b, and R.sub.8 are independently hydrogen, aryl or heteroaryl, optionally substituted by halogen, hydroxy, alkoxy, nitro, cyano and carboxy, provided that:Q.sub.3 R.sub.3 is not hydrogen or methyl in formulae (I) or (II); and at least one of R.sub.3 and R.sub.8 is aryl or heteroaryl in formula (I).The compounds are effective PDE IV inhibitors and possess improved PDE IV inhibition and improved selectivity with regard to PDE III inhibition.

Abstract: Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds possess improved PDE IV inhibition as compared to theophylline or rolipram, with improved selectivity with regard to, e.g., PDE V inhibition.

Abstract: The present invention relates to novel compounds of the formula (I): ##STR1## wherein Q.sub.3 R.sub.3 and Q.sub.8 R.sub.8 are described herein. The compounds possess PDE-IV inhibitory activity and improved selectivity with regard to PDE-III inhibition. Also disclosed are pharmaceutical compositions and methods of treatment utilizing the disclosed compounds.

Abstract: The present invention comprises methods of synthesizing compounds having the formula I: ##STR1## wherein: Y.sub.1, Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.8 are as described herein, which comprises the steps of(a) reacting a compound of the formula III ##STR2## with a base to cause cyclization to compound IV ##STR3## (b) transforming said hydroxy group of said compound IV to an amine by successive halogenation by a halogenating agent and displacement of the resultant halogen with an amide to form compound V ##STR4## (c) reacting said compound V with an effective amount of compound VI ##STR5## to form the compound of formula 1.

Abstract: The present invention comprises a method of synthesizing compounds having the formula (I): ##STR1## wherein: Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.8 are defined herein, which comprises the steps of(a) reacting a compound of the formula (II) ##STR2## wherein Q is a halogen, with an effective amount of a compound selected from the group consisting of an acid anhydride or an acid halide; to form a compound of the formula (III) ##STR3## b) transforming the 6-halo group of said compound (III) to an amine by displacement with ammonia to form compound (IV) ##STR4## (c) reacting said compound (IV) with a base to cause cyclization to a 6-halo intermediate, said 6-halo group is then transformed to an amine by displacement with an amine to form compound (V) ##STR5## (d) reacting said compound (V) with an effective amount of compound (VI) ##STR6## wherein X is a halogen; to form the compound of formula (I).