Abstract: Nanoparticles having a plurality of PVP chains covalently bonded to a surface of the nanoparticle are provided, along with their methods of formation and the RAFT agents for the polymerization of the PVP chains. RAFT agents are generally provided, along with their methods of formation and use. Methods are also generally provided for grafting a PVP polymer onto a nanoparticle. In one embodiment, the method includes: polymerizing a plurality of monomers in the presence of a RAFT agent to form a polymeric chain covalently bonded to the nanoparticle.

Abstract: The invention relates to (among other things) oligomer-foscarnet conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered un-conjugated foscarnet compounds.

Abstract: The present invention relates to a polymerization-curable composition for the preparation of biodegradable, biocompatible, cross-linked polymers on the basis of polyvinyl alcohol comprising: 5 to 100% by weight of (a) vinyl ester monomer(s) of one of the general formulas (I) to (III): wherein X is oxygen, sulfur, nitrogen, or phosphorus; n is 1 to 1000, at least 20% of the n being ?2; the R1 are selected from hydrogen; straight, branched or cyclic, saturated or unsaturated, n-valent hydrocarbon groups having 1 to 30 carbon atoms, which optionally have heteroatoms and are optionally substituted with one or more substituents selected from —OH, —COON, —CN, —CHO, and ?O, and n-valent radicals of biodegradable, biocompatible oligomers and polymers; m is an integer from 1 to 5; the R2 are selected from hydrogen, —OH, ?O, and the options listed for R1; and the R3 are selected from hydrogen, —OH, and the options listed for R1; 0 to 50% by weight of ethylenically unsaturated co-monomers; 0 to 10% by weight of (a)

Abstract: The invention relates to a process for preparing mono-carboxy-functionalized dialkylphosphinic acids, dialkylphosphinic esters and dialkylphosphinic salts by means of alkylene oxides, characterized in that a) a phosphinic acid source (I) is reacted with olefins (IV) in the presence of a catalyst A to form an alkylphosphonous acid, its salt or ester (II), b) the resultant alkylphosphonous acid, its salt or ester (II) is reacted with alkylene oxides of the formula (V) in the presence of a catalyst B, to give a mono-functionalized dialkylphosphinic acid derivative (VI), and c) the resultant mono-functionalized dialkylphosphinic acid derivative (VI) is reacted in the presence a catalyst C to give the mono-carboxy-functionalized dialkylphosphinic acid derivative (III), where R1,R2,R3,R4,R5, and R6 are identical or different and independently of one another are inter alia H, C1-C18-alkyl, C6-C18-aryl, C6-C18-aralkyl or C6-C18-alkylaryl, and X and Y are identical or different and independently of one another are H,

Abstract: The invention relates to (among other things) oligomer-foscarnet conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered un-conjugated foscarnet compounds.

Abstract: The present invention relates to a polymerization-curable composition for the preparation of biodegradable, biocompatible, cross-linked polymers on the basis of polyvinyl alcohol comprising: 5 to 100% by weight of (a) vinyl ester monomer(s) of one of the general formulas (I) to (III): wherein X is oxygen, sulfur, nitrogen, or phosphorus; n is 1 to 1000, at least 20% of the n being ?2; the R1 are selected from hydrogen; straight, branched or cyclic, saturated or unsaturated, n-valent hydrocarbon groups having 1 to 30 carbon atoms, which optionally have heteroatoms and are optionally substituted with one or more substituents selected from —OH, —COON, —CN, —CHO, and ?O, and n-valent radicals of biodegradable, biocompatible oligomers and polymers; m is an integer from 1 to 5; the R2 are selected from hydrogen, —OH, ?O, and the options listed for R1; and the R3 are selected from hydrogen, —OH, and the options listed for R1; 0 to 50% by weight of ethylenically unsaturated co-monomers; 0 to 10% by weight of (a)

Abstract: Disclosed are water soluble dithioesters capable of acting as chain transfer agents in preparing a vinyl-based polymer to control molecular weight and molecular weight distribution thereof as well as being capable of living polymerization even in an aqueous solution, and a method for polymerization thereof.

Abstract: Disclosed are water soluble dithioesters capable of acting as chain transfer agents in preparing a vinyl-based polymer to control molecular weight and molecular weight distribution thereof as well as being capable of living polymerization even in an aqueous solution, and a method for polymerization thereof.

Abstract: Preparations of pyrophosphate analogues, including phosphonoformic acid, bisphosphonic acid, and phosphonoacetic acid derivatives, exhibiting antiviral activity. Such compounds, are used directly, or as prodrugs, in compositions and methods for treating viral infections, including but not limited to HIV, herpesviruses including HSV, EBV, VZV, CMV, HHV-6 and HHV-8 (Kaposi's sarcoma); HPV; rhinoviruses; and hepatitis-linked viruses. Compounds of the present invention for use as antiviral agents or their intermediates include sulfur-containing, polyhydroxy, and lipophilic derivatives of phosphonoformic acid.

Abstract: Preparation of phosphonoformic acid analogues containing one, two, three, or more sulfur atoms are described, with specific examples. Such compounds, not excluding cognates, derivatives, and homologues thereof, are proposed to be used directly, or as prodrugs, in treating viral infections, including but not limited to HIV, herpesviruses including HSV, EBV, VZV, CMV, HSV-6 and HSV-8 (Kaposi's sarcoma); HPV; rhinoviruses; and hepatitis-linked viruses. They are also proposed to be used in treating neoplasms, and for diagnosis and therapy of diseases of bone metabolism. The compounds of the present invention are also designed as to create novel biologically active compounds or prodrugs.

Abstract: The present invention concerns new lipid derivatives of phosphonocarboxylic acids of the general formula I, ##STR1## in which the meaning of the symbols is elucidated in the description, tautomers thereof and their physiologically tolerated esters and salts of inorganic or organic bases as well as processes for the production thereof and pharmaceutical agents containing these compounds.

Abstract: Lipid prodrugs of phosphonoacids and their analogs that have increased antiviral activity over the parent drugs in inhibiting cytomegalovirus and other susceptible viruses.

Abstract: Compounds of formula (I), ##STR1## wherein R is a biphenyl group optionally substituted, by one or more substituents, the same or different selected among halogen atoms, hydroxy groups, alkoxy, alkyl thioalkyl or alkoxycarbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety, C.sub.1 -C.sub.3 alkyl groups containing one or more fluorine atoms, carboxy groups, nitro groups, amino or aminocarbonyl groups, acylamino groups, aminosulphonyl groups, momo- or di-alkylamino groups having from 1 to 6 carbon atoms in the alkyl moiety, mono- or di-alkylamino-carbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety; R.sub.1 is a hydrogen atom, a straight or branched C.sub.1 -C.sub.

Abstract: Novel phosphorus containing compounds are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful in preventing the intestinal absorption of cholesterol and thus are useful in the treatment of hypercholesterolemia and atherosclerosis.

Abstract: Compounds are disclosed for treating viral infections due to herpes, influenza, hepatitis B, Epstein-Barr, and varicella zoster viruses, as well as cytomegalovirus and human immunodeficiency virus (HIV) by means of lipid derivatives of antiviral agents. The compounds consist of lipid derivatives of phosphonoacids having antiviral activity which are linked, commonly through the phosphate group of the phosphonoacid, to one of a selected group of lipids.The lipophilic nature of these compounds provides advantages over the use of the phosphonoacids alone. It also makes it possible to incorporate them into the lamellar structure of liposomes when combined with similar molecules. In the form of liposomes, these antiviral molecules are preferentially taken up by macrophages and monocytes, cells which have been found to harbor the target human immunodeficiency virus (HIV).

Abstract: Methods for converting phosphonates into thiophosphonates and specific thiophosphonate compounds so produced are disclosed and claimed. The methods start with a reaction mixture formed of a phosphonate compound, including one or more strong electron-withdrawing groups located adjacent to the phosphorus in the compound, a slight excess of Lawesson's reagent, and a polar aprotic solvent. The reaction mixture is heated until reaction is complete and may be followed with separation or hydrolyzation steps to produce thiophosphonic acids and their addition salts. One of these thio-analogues, thiophosphonoformic acid (TPFA) is particularly effective at inhibiting HIV replication and in treating HIV infection.

Abstract: Compounds which are inhibitors of cholesterol biosynthesis (by inhibiting de novo squalene biosynthesis), and thus are useful as hypocholesterolemic agents and antiatherosclerotic agents, are provided which have the structure ##STR1## wherein R.sup.2 is a metal ion, lower alkyl or H;R.sup.3 is a metal ion or lower alkyl;R is R.sup.1 --(CH.sub.2).sub.n --, R.sup.1 --(CH.sub.2).sub.m --O-- orR.sup.1 --(CH.sub.2).sub.m --OCH.sub.2 --, wherein n is 1 to 4 and m is 0 to 3, andR.sup.1 is R.sup.5 --Q.sup.1 --Q.sup.2 --Q.sup.3 --wherein R.sup.5, Q.sup.1, Q.sup.2 and Q.sup.3 are as defined herein.New intermediates, new methods of preparation and a method for using such compounds to inhibit cholesterol biosynthesis are also provided.

Abstract: Compounds which are inhibitors of cholesterol biosynthesis (by inhibiting de novo squalene biosynthetis), and thus are useful as hypocholesterolemic agents and antiatherosclerotic agents, are provided which have the structure ##STR1## wherein R.sup.2 is a metal ion, lower alkyl or H; R.sup.3 is a metal ion or lower alkyl;R is R.sup.1 --(CH.sub.2).sub.n --, R.sup.1 --(CH.sub.2).sub.m --O-- orR.sup.1 --(CH.sub.2).sub.m --OCH.sub.2 --, wherein n is 1 to 4 and m is 0 to 3, andR.sup.1 is R.sup.5 --Q.sup.1 --Q.sup.2 --Q.sup.3 -- wherein R.sup.5, Q.sup.1, Q.sup.2 and Q.sup.3 are as defined herein.New intermediates, new methods of preparation and a method for using such compounds to inhibit cholesterol biosynthesis are also provided.

Abstract: A novel phosphonamidothionate derivative represented by the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined in the disclosure. The present novel compound has excellent properties with respect to not only pesticidal activity but also maintenance of the pesticidal activity over a prolonged period of time after application. The present novel compound can be prepared by a new unique process in which the direct phosphorylation of a carbamate compound is involved.