Abstract: This invention relates to compounds, pharmaceutical compositions, and methods of using compounds of the formula: or a pharmaceutically acceptable salt, hydrate, prodrug, or mixtures thereof, wherein Y is alkylhalo, alkyl-CO—G, COG, a direct bond, C═O, O, NR11, or CR8; G is NR11R16, OR9, SR9, or R10; Z is O, S, or NR11; X is NR16, O, S, CR12R13, C═O, a bond, —CR12═CR13—, —C(R12R13)C(R14R15)—, or; Rhd 1, R2, R3, R4, R5, R6, R7, R8, R10, R12, R13, R14, or R15 are independently: hydrogen, halo, alkylhalo, hydroxy, C1-C9 straight or branched chain alkyl, C2-C9 straight or branched chain alkenyl group, C3-C8 cycloalkyl, C5-C7 cycloalkenyl, aryl, amino, alkylamino, nitro, nitroso, carboxy, or aralkyl; R9 is hydrogen, hydroxy, C1-C9 straight or branched chain alkyl, C2-C9 straight or branched chain alkenyl group, C3-C8 cycloalkyl, C5-C7 cycloalkenyl, aryl, amino, alkylamino, carboxy, or aralkyl; R11 or R16 are independently: hydrogen, halo, alkylha

Abstract: This invention relates to neurotrophic compounds having an affinity for FKBP-type immunophilins, their preparation and use as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity.

Abstract: A medical device is described comprising a biodegradable terephthalate copolymer comprising the recurring monomeric units shown in formula I: wherein R is a divalent organic moiety; R′ is an aliphatic, aromatic or heterocyclic residue; x is ≧1; and n is 3-7, 500, where the biodegradable polymer is sufficiently pure to be biocompatible and is capable of forming biocompatible residues upon biodegradation. Compositions containing the copolymers and biologically active substances, articles useful for implantation or injection into the body fabricated from the compositions, and methods for controllably releasing biologically active substances using the copolymers, are also described.

Abstract: Biodegradeable polymer compositions suitable for intraperitoneal administration to treat a mammalian subject having ovarian cancer are described, wherein the polymer compositions provide extended release of the antineoplastic agent into the peritoneum of the subject. The subject compositions can increase the median survival rate from the cancer by at least about 10%, as compared with the median survival rate obtained by administration of a composition comprising the same dosage of the antineoplastic agent without the biodegradeable polymer. Solid articles and methods for treating ovarian cancer are also described.

Abstract: The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives that inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, and to treat prostate diseases, especially using the compounds of the present invention for the inhibition of the growth of prostate cancer cells.

Abstract: A compound of formula I: 1

Abstract: A compound of formula I: 1

Abstract: The present invention relates to N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) inhibitors enzyme activity, pharmaceutical compositions comprising such inhibitors, and methods of their use to inhibit NAALADase enzyme activity, thereby effecting neuronal activities, inhibiting angiogenesis, and treating glutamate abnormalities, compulsive disorders, prostate diseases, pain and diabetic neuropathy.

Abstract: The present invention provides improved processes for purifying polymer preparations by removing contaminants, such as metal contaminants. The present invention also provides improved processes for producing phosphopolymers, which can yield improved polymers in terms of molecular weight, homogeneity, consistency and purity. Polymers and polymer preparations also are provided. The present invention is time, labor and energy efficient, and thus marks an improvement over past approaches.

Abstract: New benzenedicarboxylic acid derivative compounds; pharmaceutical compositions, diagnostic methods, and diagnstic kits that include those compounds; and methods of using those compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, neutopathy, pain, compulsive disorders, prostate diseases, cancers, and glaucoma.

Abstract: Process for the preparation of radiohalogenated radiopharmaceuticals by an electrophillic substitution, preferably halogenodestannylation reactions, by the reaction of an organometallic substituted precursor, preferably a trialkyl tin substituted precursor, with a radioactive halogen, preferably a radioactive iodine, astatine or bromine composition, in the presence of a catalytically effective amount of an anion selected from the group consisting of bromide, chloride and nitrite anion in an acid medium with an oxidizing agent.

Abstract: This invention relates to the method of using neurotrophic cyclophilin inhibitor compounds having an affinity for cyclophilin-type immunophilins as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity.

Abstract: The present invention relates to methods of using NAALADase inhibitors to regulate TGF-&bgr; and to treat neurodegenerative disorders, extracellular matrix formation disorders, cell-growth related diseases, infectious diseases, immune related diseases, epithelial tissue scarring, collagen vascular diseases, fibroproliferative disorders, connective tissue disorders, inflammatory diseases, respiratory distress syndrome and infertility.

Abstract: A compound of formula I: or a pharmaceutically acceptable salt, prodrug, metabolite, optical isomer or stereoisomer thereof, wherein: R1, when present, is hydrogen or lower alkyl; R2 is lower alkyl, aryl, aralkyl, lower alkanoyl, or —(CH2)n—(CHOH)y(CH2)mA, wherein n is 1-4, y is 0 or 1, m is 0-5, and A is cycloalkyl, cycloalkenyl, lower alkanoyl, aryl, aralkyl, —NH2, —NH-(lower alkyl), Y represents the atoms necessary to form a fused 5- to 6-membered ring that is aromatic or nonaromatic and carbocyclic or heterocyclic; Z is (i) —CHR2CHR3— where R2 and R3 are independently hydrogen, alkyl, aryl or aralkyl; (ii) —R6C═CR3— where R6 and R3 are independently hydrogen, lower alkyl, aryl, aralkyl, chlorine, bromine or —NR7R8, where R7 and R8 are independently hydrogen or lower alkyl, or, R6 and R3, taken together, form a fused 5- to 6-membered ring that is aromatic or nonaromatic and carbocyclic or heterocyclic; (iii

Abstract: An essentially non-osteoconductive medical device is described comprising a biodegradable terephthalate copolymer comprising the recurring monomeric units shown in formula I: wherein R is a divalent organic moiety; x is ≧1; and n is 3-7,500, where the biodegradable polymer is sufficiently pure to be biocompatible and is capable of forming biocompatible residues upon biodegradation. Compositions containing the copolymers and biologically active substances, articles useful for implantation or injection into the body fabricated from the compositions, and methods for controllably releasing biologically active substances using the copolymers, are also described.

Abstract: The present invention relates to a method of treating a glutamate abnormality and a method of effecting a neuronal activity in an animal using a NAALADase inhibitor, and a pharmaceutical composition comprising an effective amount of a NAALADase inhibitor for treating a glutamate abnormality and effecting a neuronal activity in an animal.

Abstract: Biodegradable, flowable or flexible polymer compositions are described comprising a polymer having the recurring monomeric units shown in formula I: wherein: each of R and R′ is independently straight or branched alkylene, either unsubstituted or substituted with one or more non-interfering substituents; L is a divalent cycloaliphatic group; R″ is selected from the group consisting of H, alkyl, alkoxy, aryl, aryloxy, heterocyclic or heterocycloxy; and n is 5 to 1,000, wherein said biodegradable polymer is biocompatible before and upon biodegradation. In one embodiment, one or more of R, R′ or R″ is a biologically active substance. Amorphous compositions containing a biologically active substance, in addition to the polymer, and methods for controllably releasing biologically active substances using the compositions, are also described.

Abstract: The present invention provides carboxamine compounds, methods and compositions for inhibiting PARP activity.

Abstract: The present disclosure relates to a method of inhibiting angiogenesis comprising administering a N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) inhibitor to a patient in need thereof, and a pharmaceutical composition comprising an anti-angiogenic effective amount of a NAALADase inhibitor and a pharmaceutically acceptable carrier.

Abstract: This invention relates to compounds, pharmaceutical compositions, and methods of using compounds of the formula: wherein R1-R9 and Z are independently. hydrogen, hydroxy, halo, haloalkyl, thiocarbonyl, cyano, nitro, amino, imino, alkylamino, aminoalkyl, sulfhydryl, thioalkyl, alkylthio, sulfonyl, alkylsulfonyl, C1-C9 straight or branched chain alkyl, C2-C9 straight or branched chain alkenyl, C2-C9 straight or branched chain alkynyl, C1-C6 straight or branched chain alkoxy, C2-C6 straight or branched chain alkenoxy, C2-C6 straight or branched chain alkynoxy, aryl, carbocycle, heterocycle, aralkyl, alkylaryl, alkylaryloxy, aryloxy, aralkyloxy, aralkylsulfonyl, aralkylamino, arylamino, arylazo, arylthio, or aralkylthio; or Z is wherein U is C or N, and R7 and R8 are defined above; and X and Y are independently aryl, carbocycle, or heterocycle.