Abstract: Methods of synthesizing a substantially monodispersed mixture of polymers comprising polyethylene glycol moieties include: reacting a substantially monodispersed mixture of compounds having the structure of Formula I: R1(OC2H4)n—O−X+  (I) wherein R1 is H or a lipophilic moiety; n is from 1 to 25; and X+ is a positive ion,  with a substantially monodispersed mixture of compounds having the structure of Formula II: R2(OC2H4)m—OMs  (II) wherein R2 is H or a lipophilic moiety; and m is from 1 to 25, under conditions sufficient to provide a substantially monodispersed mixture of polymers comprising polyethylene glycol moieties and having the structure of Formula III: R2(OC2H4)m+n—OR1  (III).

Abstract: Mixtures of conjugates in which each conjugate in the mixture comprises a growth hormone drug coupled to an oligomer that includes a polyalkylene glycol moiety wherein the mixtures have a molecular weight distribution with a standard deviation of less than about 22 Daltons are disclosed. Methods of treating growth hormone deficiency in a subject in need of such treatment and methods of accelerating the growth rate of an animal arc also disclosed. Processes for synthesizing substantially monodispersed mixtures of conjugates wherein each conjugate comprises a growth hormone drug coupled to an oligomer that comprises a polyethylene glycol moiety are further provided.

Abstract: A mixture of conjugates in which each conjugate in the mixture comprises an insulin drug coupled to an oligomer that includes a polyalkylene glycol moiety is disclosed. The mixture may exhibit higher in vivo activity than a polydispersed mixture of similar conjugates. The mixture may also be more effective at surviving an in vitro model of intestinal digestion than polydispersed mixtures of similar conjugates. The mixture may also result in less inter-subject variability than polydispersed mixtures of similar conjugates.

Abstract: Methods of synthesizing a substantially monodispersed mixture of polymers comprising polyethylene glycol moieties include: reacting a substantially monodispersed mixture of compounds having the structure of Formula I: R1(OC2H4)n—O−X+  (I) wherein R1 is H or a lipophilic moiety; n is from 1 to 25; and X+ is a positive ion, with a substantially monodispersed mixture of compounds having the structure of Formula II: R2(OC2H4)m—OMS  (II) wherein R2 is H or a lipophilic moiety; and m is from 1 to 25, under conditions sufficient to provide a substantially monodispersed mixture of polymers comprising polyethylene glycol moieties and having the structure of Formula III: R2(OC2H4)m+n—OR1  (III). Substantially monodispersed mixtures of polymers comprising polyethylene glycol moieties are also disclosed.

Abstract: Methods of synthesizing an acylanilide include contacting a compound having the structure of Formula I: with a compound having the structure of Formula II: under conditions sufficient to provide a compound having the structure of Formula III: and treating the compound of Formula III under conditions sufficient to provide an acylanilide.

Abstract: Pharmaceutical compositions that include a drug-oligomer conjugate, a fatty acid component, and a bile salt component are described. The drug is covalently coupled to an oligomeric moiety. The fatty acid component and the bile salt component are present in a weight-to-weight ratio of between 1:5 and 5:1. Methods of treating diseases in a subject in need of such treatment using such pharmaceutical compositions are also provided, as are methods of providing such pharmaceutical compositions.

Abstract: The present invention provides compositions useful for the treatment of inflammation in humans, and related methods of treatment for the same. In one embodiment the composition is: In another embodiment, the composition is: In yet another embodiment, the composition is: Additional alternative embodiments are R or R″ are therapeutic moieties.

Abstract: The present invention provides amphiphilic prodrugs comprising a therapeutic compound conjugated to an PEG-oligomer/polymer and methods for using said prodrugs to enable oral drug delivery and/or delivery of drugs across the blood brain barrier into the central nervous system.

Abstract: A mixture of conjugates in which each conjugate in the mixture comprises a calcitonin drug coupled to an oligomer that includes a polyalkylene glycol moiety is disclosed. The mixture may lower serum calcium levels in a subject by 10, 15 or even 20 percent or more. Moreover, the mixture may be more effective at surviving an in vitro model of intestinal digestion than non-conjugated calcitonin. Furthermore, the mixture may exhibit a higher bioavailability than non-conjugated calcitonin.

Abstract: The present invention provides compositions useful for the treatment of inflammation in humans, and related methods of treatment for the same. In one embodiment the composition is In another embodiment, the composition is Additional alternative embodiments are R or R″ that are therapeutic moieties.

Abstract: The present invention relates to amphiphilic drug-oligomer conjugates capable of traversing the blood-brain barrier (“BBB”) and to methods of making and using such conjugates. An amphiphilic drug-oligomer conjugates comprise a therapeutic compound conjugated to an oligomer, wherein the oligomer comprises a lipophilic moiety coupled to a hydrophilic moiety. The conjugates of the invention further comprise therapeutic agents such as proteins, peptides, nucleosides, nucleotides, antiviral agents, antineoplastic agents, antibiotics, etc., and prodrugs, precursors, derivatives and intermediates thereof, chemically coupled to amphiphilic oligomers.

Abstract: The present invention provides compositions useful for the treatment of inflammation in humans, and related methods of treatment for the same. In one embodiment the composition is In another embodiment, the composition is Additional alternative embodiments are R or R″ that are therapeutic moieties.

Abstract: Proteins and/or peptides, such as luminal cholecystokinin releasing factor (LCRF), are conjugated with amphiphilic oligomers and polymers. Such conjugates may modulate the pharmacokinetic profile and/or peptides; thereby improving their clinical utility. Such conjugates may also stabilize and deliver the proteins and/or peptides, such as LCRF, to receptors in the gut without absorption into the bloodstream.

Abstract: The present invention provides compositions useful for the treatment of inflammation in humans, and related methods of treatment for the same. In one embodiment the composition is In another embodiment, the composition is Additional alternative embodiments are R or R″ that are therapeutic moieties.

Abstract: A methods of preparing a substantially pure enantiomer of an acylanilide such as Casodex® (bicalutamide) and/or its derivatives includes resolving an intermediate compound having the structure of Formula I: wherein R1 is alkyl or haloalkyl having up to 4 carbons; R2 is alkyl having up to 6 carbon atoms; R3 is a direct link or alkyl having up to 6 carbon atoms; R4 is alkyl, alkenyl, hydroxyalkyl or cycloalkyl each of up to 6 carbons; or R4 is phenyl which bears one, two or three substituents independently selected from hydrogen, halogen, nitro, carboxy, carbamoyl and cyano, and alkyl, alkoxy, alkanoyl, alkylthio, alkylsulphinyl, alkylsulphonyl, perfluoroalkyl, perfluoroalkylthio, perfluoroalkylsulphinyl, perfluoroalkylsulphonyl, alkoxycarbonyl and N-alkylcarbamoyl each of up to 4 carbon atoms, and phenyl, phenylthio, phenylsulphinyl and phenylsulphonyl; or R4 is naphthyl; or R4 is a 5- or 6-membered saturated or unsaturated heterocyclic which contains one, two or three heteroatoms sel

Abstract: Methods of synthesizing pure enantiomers of acylanalides such as Casodex® (bicalutamide) and its derivatives utilizing a compound having a ring structure that, when opened, provides a substituent having the structure of Formula I: wherein R1 is alkyl or haloalkyl having up to 4 carbons; R2 is alkyl having up to 6 carbon atoms; and R3 is CH2OR4 where R4 is hydrogen or benzyl, C(O)CH3, or C(O)OR5 where R5 is hydrogen or alkyl; are disclosed. Methods of synthesizing acylanalides such as Casodex® (bicalutamide) and/or derivatives thereof from a starting material of citramalic acid are also provided.

Abstract: Compounds are disclosed having the structure of Formula I: where R1, R3, and R4 are independently hydrogen or C1 to C4 alkyl, and R2 is: where R5 is selected from the group consisting of hydrogen and C1 to C4 alkyl, or where R6, R7 and R8 are independently hydrogen or C1 to C4 alkyl; or the esters or pharmacologically acceptable salts thereof. Such compounds may be utilized for the prophylaxis or treatment of various diseases, particularly inflammatory conditions of the GI tract. Methods of treating inflammatory conditions of the GI tract such as inflammatory bowel disease using compounds having the following formula are also disclosed: where R9, R10 and R11 are independently selected from the group consisting of hydrogen and C1 to C4 alkyl, and R12 is selected from the group consisting of hydrogen and —C(O)R13, where R13 is a C1 to C6 alkyl or an aryl group.

Abstract: The invention generally relates to a new gene probe biosensor employing near field surface enhanced Raman scattering (NFSERS) for direct spectroscopic detection of hybridized molecules (such as hybridized DNA) without the need for labels, and the invention also relates to methods for using the biosensor.

Abstract: The present invention relates to &bgr;-hCG, particularly &bgr;-hCG proteins having a sequence of amino acids 41-54, 45-54, 47-53, 45-57 and 45-58 and analogs and derivatives thereof. The invention further relates to methods of treatment and prevention of HIV infection by administration of a therapeutic compound of the invention. Such therapeutic compounds include hCG, &bgr;-hCG and &bgr;-hCG peptides, analogs and derivatives of hCG, &bgr;-hCG and &bgr;-hCG peptides, and nucleic acids encoding hCG, &bgr;-hCG and &bgr;-hCG peptides. In a preferred embodiment, &bgr;-hCG peptides, particularly &bgr;-hCG peptides of amino acids 47-53, 45-57 or 45-58 are administered to a subject for treatment or prevention of HIV infection in that subject. The invention also provides methods for screening hCG preparations for activity in treating or preventing HIV infection. Pharmaceutical compositions and methods of administration of Therapeutics are also provided.

Abstract: The invention relates to a membrane system for controlled tissue regeneration of the periodontium, comprising a resorbable polymer membrane and anti-adhesion molecules.