Abstract: The present invention provides phosphonate conjugates and methods of preparing the phosphonate conjugates so as to allow, for example, improved methods and compounds for modifying the surface of a nanoparticle to increase in vivo circulation times and targeted delivery performance.

Abstract: The present invention provides novel compounds and pharmaceutical compositions for the prevention and/or treatment of cancer and precancerous conditions thereof, for the treatment of pain and fever, for the treatment of skin disorders, and for treating and/or preventing inflammation-related diseases and/or cardiovascular diseases. The compounds of the invention also have analgesic properties and anti-platelet properties. The compounds of the invention may be provided to animals, including mammals and humans, by administering a suitable pharmaceutical dose in a suitable pharmaceutical dosage form. The compounds of the invention have improved efficacy and safety, including higher potency and/or fewer or less severe side effects, than conventional therapies. The compounds of the invention comprise a biologically active moiety or portion (A) that has, or is modified to have at least one carboxyl group.

Abstract: Novel compounds and pharmaceutical compositions thereof for the treatment and/or prevention of cancer and precancerous conditions, inflammation-related disorders, pain and fever.

Abstract: A chelating agent, a metal-chelate, and a contrast agent are provided, wherein the chelating agent comprises a compound of structure (I) wherein R1, R2, R3, R8, R7, R?7 R?1, R?2, R?3 and R8? are selected from a hydrogen, a protected C1-C3 hydroxyalkyl group, a C1-C3 alkyl group; R4 and R?4 are selected from a hydrogen, a hydroxyl group, a protected hydroxy group, a protected C1-C3 hydroxyalkyl group, a C1-C3 alkyl group; n is an integer between 0 and 4; R5 and R?5 are selected from a hydrogen, a protecting group selected from the group consisting of C1-C30 aliphatic radicals, C3-C30 cycloaliphatic radicals, C2-C30 aromatic radicals; R9 and R?9 are selected form a hydrogen or a protecting group selected from the group consisting of C1-C30 aliphatic radicals, C3-C30 cycloaliphatic radicals, C2-C30 aromatic radicals, m is an integer between 0 and 10; and at least one of R7 and R?7 is acidic group or a protected acidic group.

Abstract: Substituted saccharide compounds, dental compositions comprising substituted saccharide compounds, and methods of using dental compositions are described. In one embodiment, the substituted saccharide amide compound comprises a hydrophobic group and at least one free-radically polymerizable group with the proviso that the hydrophobic group is not bonded to the ethylenically unsaturated carbon atom of the free-radically polymerizable group. The hydrophobic group is typically bonded to a nitrogen atom of a saccharide amine residue or a carbonyl moiety of saccharide amide residue.

Abstract: A phospholipid derivative represented by the following formula (1) wherein each symbol is as described in the specification; a liposome containing the phospholipid derivative, and the like.

Abstract: The present invention provides phosphonate conjugates and methods of preparing the phosphonate conjugates so as to allow, for example, improved methods and compounds for modifying the surface of a nanoparticle to increase in vivo circulation times and targeted delivery performance.

Abstract: Provided herein are monomers incorporating folate or other targeting agent, polymers prepared therefrom, polymers prepared therefrom having a therapeutic agent covalently coupled thereto, as well as micelles and therapeutic compositions thereof.

Abstract: The present invention relates to compounds and methods useful in the prevention or treatment of diseases or conditions associated with Toll-like receptor 2 activation.

Abstract: The present invention is directed to methods of treating diseases and disorders related to immune responses by administering one or more immunomodulatory compounds. In particular, the invention is directed to methods of stimulating and reducing immune responses, therapeutic and prophylactic treatment of cancer, treating autoimmune conditions, treating allergic reactions and asthma, and preventing ischemic damage and asthma by administering one or more immunomodulatory compounds.

Abstract: Novel phosphonate compounds are disclosed embodying an aminophosphonate moiety and a selected reaction partner. These compounds offer beneficial alternatives, and additional possibilities, to extant phosphonates and are capable of delivering desirable benefits from an application standpoint and from a compatibility standpoint broadly.

Abstract: Disclosed is a phosphate transport inhibiting compound represented by Structural Formula (I): R1 and R2 are independently —H, an electron withdrawing group or a C1–C10 alkyl group. Y is a covalent bond, a substituted methylene group, an unsubstituted methylene group or —CR1R2P(O)(OH)—. R3 is a hydrocarbyl group optionally comprising one or more amine, ammonium, ether, thioether or phenylene linking groups, a substituted hydrocarbyl group optionally comprising one or more amine, ammonium, ether, thioether or phenylene linking groups, a heteroaryl group, a substituted heteroaryl group or a phenyl group substituted with one or more groups selected from —Cl, —Br, —F, —CN, —NO2, —ORa, —N(Ra)2, —COORa, —CON(Ra)2, —CORa, —S(O)Ra, —S(O)2Ra, —S(O)2N(Ra)2, —NRaS(O)2Ra, —NRaCORa, a halogenated lower alkyl group, an aryl group, a substituted aryl group, or a halogenated alkoxy group. Each Ra is independently —H, lower alkyl, substituted lower alkyl, aryl or substituted aryl.

Abstract: This invention describes a new method of constructing double-stranded DNA (dsDNA) microarrays based on the use of pre-synthesized or natural DNA duplexes without a stem-loop structure. The complementary oligonucleotide chains are bonded together by a novel connector that includes a linker for immobilization on a matrix. A non-enzymatic method for synthesizing double-stranded nucleic acids with this novel connector enables the construction of inexpensive and robust dsDNA/dsRNA microarrays. DNA-DNA and DNA-protein interactions are investigated using the microarrays.

Abstract: This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediate by one or more molecular interactions involving a phosphotyrosine-containing protein. This invention also relates to pharmaceutic compositions containing the compounds and prophylactic and therapeutic methods involving pharmaceutical and veterinary administration of the compounds. The compounds are of formula (1) as defined herein.

Abstract: The present invention provides novel compounds that function as immunological adjuvants when co-administered with antigens, including, antigens used as vaccines for any disease or condition amenable to vaccination. The invention also provides adjuvant formulations comprising the novel compounds of the invention and methods for immunizing humans and non-human animals.

Abstract: The invention includes compositions and methods useful for treatment of a virus infection in a mammal by double-targeting the virus (i.e. targeting the virus at more than one stage of the virus life cycle) and thereby inhibiting virus replication. The compositions of the invention include compounds, which comprise a phosphocholine moiety covalently conjugated with one or more therapeutic agents (e.g. nucleoside analogue, protease inhibitor, etc.) to a lipid backbone. The invention also includes pharmaceutical compositions for use in treatment of a virus infection in mammals. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt or a prodrug thereof, or a pharmaceutical composition of the invention, in an amount effective to treat the infection, to a mammal infected with a virus.

Abstract: Compounds having utility in achieving the foregoing objects of the invention are prepared by reacting a 2,2-bis-(disubstituted-phosphoryl)-ethylsulfanyl-acetic acid compound with a pharmaceutically active chemical entity effective to treat the underlying disease state or with non-pharmaceutical entities such as pesticides, insecticides, fungicides or poisons for vermin.

Abstract: The present invention is directed to novel compounds that function as immunological adjuvants when co-administered with antigens such as vaccines for bacterial and viral diseases, to novel adjuvant formulations which include at least one of the adjuvant compounds of the invention, to novel immunostimulatory compositions which comprise an antigen and at least one of the adjuvant compounds of the invention, and to methods for the immunization of an animal by co-administration of a compound of the invention with an antigen against which the animal is to be immunized.

Abstract: The present invention provides crosslinking, conjugating and reducing agents which are functional with at least one phosphorothioate monoester group (--SPO.sub.3.sup.-2). Crosslinking and conjugation methods as well as solid phase reagents and conjugates which are useful in immunoassays are also provided.Crosslinking and conjugating agents of the invention generally comprise a compound corresponding to the formula (I), shown below, wherein n at least 1 and Q is a straight or branched monomer, polymer or oligomer having an average molecular weight between about 200 and about 1,000,000. Additionally, when n is 1, Q comprises at least 1 additional reactive functionality.Q--(S--PO.sub.3.sup.-2).sub.n (I)The reducing agents that are provided conform to a compound of the formula (Y), shown below, wherein (A) and (Z) can be independently selected from C.sub.1 -C.sub.5 alkyl and CONH(CH.sub.2).sub.p wherein p is an integer between 1 and 5.

Abstract: A phosphorus ester oligomer having the structure: wherein A can be the same or different in each monomeric unit and each is independently selected from the group consisting of oxygen, sulfur, lower alkyl, substituted or unsubstituted alkylamino, substituted or unsubstituted arylamino and aminoalkyl; B.sub.1 and B.sub.2 can be the same or different and each is independently selected from hydrogen, lower alkyl, a labeling group, a protecting group, a phosphoramidate or a phosphomonoester; R.sub.1 can be the same or different in each monomeric unit, and in at least one of the non-nucleotide monomeric units, R.sub.

Abstract: A novel estrogen derivative represented by the formula: ##STR1## is useful for treating or preventing diseases caused by estrogen deficiency.

Abstract: Cyclic and acyclic 2-aminopurine phosphonate nucleotide analogs useful to treat herpes viral infections are provided in enantiomerically pure form. Pharmaceutical compositions and methods for treating herpes viral infections are provided as well, as is a chiral synthesis for preparing the novel compounds in enantiomerically pure form.

Abstract: Inks, particularly inks for ink jet printing, contain at least one compound of the formula I ##STR1## as a stabilizer. The symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.3 ' and R.sub.4 ' are as defined in claim 1. The compounds are in part novel and are suitable for use as light stabilizers for organic materials.

Abstract: Chemically-defined, non-polymeric valency platform molecules and conjugates comprising chemically-defined valency platform molecules and biological or chemical molecules including polynucleotide duplexes of at least 20 base pairs that have significant binding activity for human lupus anti-dsDNA autoantibodies.

Abstract: Novel bis(aminomethyl)phosphinic acid derivatives and process for the preparation of bis(aminomethyl)phosphinic acid derivativesCompounds of the formula VI ##STR1## can be prepared by reaction of a compound of the formula IV ##STR2## with a base to give a compound of the formula Va or Vb ##STR3## and subsequent reaction with carbon nucleophiles; alternatively the compound of the formula VI is prepared by direct reaction of the compound of the formula IV e.g. with R.sup.2 Cu(CN)Li.sub.2, the above substituents having the meanings mentioned.

Abstract: Diphosphonic acids of formula (I) are useful as antitumor agents.

Abstract: Diphosphonic acids of formula (I) are disclosed. These compounds are useful as antitumor agents.

Abstract: Novel pharmacologically active methylenebisphosphonates having formula (I) wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently are straight or branched, optionally unsaturated C.sub.1 -C.sub.10 -alkyl, optionally unsaturated C.sub.3 -C.sub.10 -cycloalkyl, aryl, aralkyl, silyl SiR.sub.3 or hydrogen, whereby in formula (I) at least one of the groups R.sup.1, R.sup.2, R.sup.3 or R.sup.4 is hydrogen and at least one of the groups is different from hydrogen, Q.sup.1 is hydrogen, hydroxyl, halogen, amino NH.sub.2, or OR', wherein R' is C.sub.1 -C.sub.4 -lower alkyl or acyl, Q.sup.2 is straight or branched, optionally unsaturated C.sub.1 -C.sub.10 -alkyl, -hydroxyalkyl or -aminoalkyl, whereby the oxygen may, as a substituent, contain one group or the nitrogen as a substituent may contain one or two groups, which are C.sub.1 -C.sub.4 -lower alkyl or acyl, or the two substituents of the nitrogen form together with the nitrogen atom a saturated, partly saturated or an aromatic heterocyclic ring, or Q.sup.

Abstract: Modified ceramides are defined, together with their synthesis and compositions comprising them for topical application to human skin, hair and nails. The modified pseudoceramides have a structure: ##STR1## and an approximate summary is that R and R.sup.1 are aliphatic hydrocarbon, A is CH.sub.2, CHOR.sup.2, CH.dbd.CH or CHOY, and at least one of R.sup.2, R.sup.3 and R.sup.4 is sulphate, phosphate or similar. The presence of phosphate or sulphate facilitates skin absorption, after which the phosphate or sulphate is removed by enzymes present in vivo.

Abstract: There is disclosed a group of lubricant additives that have improved oxidative stability, high viscosity and relatively lower cost and that comprise telomerized vegetable oils having no more than 4% polyunsaturated fatty acids. There is also disclosed sulfurized and phosphite adduct derivatives of telomerized vegetable oil for use as lubricant additives.

Abstract: Compounds of the tautomeric formula Ia, Ib or Ic, ##STR1## where R is a radical of the formula ##STR2## are effective compounds for the treatment and prophylaxis of degenerative bone disorders. They are used as pharmaceuticals.

Abstract: Onium salt capable of generating acid upon exposure to actinic radiation having the following structure:(R.sub.1).sub.a (R.sub.2).sub.b (R.sub.3).sub.c Q.sup.+ --A--M.sup.+ X.sup.- --B--X'.sup.-where:Q is S;R.sub.1, R.sub.2 and R.sub.3 are independently substituted or unsubstituted aromatic, aliphatic, or aralkyl groups having 7-18 carbon atoms;M.sup.+ is a cationic organic radical;A is a divalent radical selected from the group of hindered alkylene groups, substituted or unsubstituted aromatic or aralkyl groups;B is a divalent aromatic sensitizer which absorbs radiation having a wavelength longer than 300 nm and is capable of transferring an electron to Q,x.sup.- and X'.sup.- are anionic groups; and wherein A provides a spatial separation between Q and M, and B provides a spatial separation between X and X', such that the spatial separation provided by A between Q and M is substantially the same as the spatial separation provided by B between X and X'.

Abstract: Diphosphonic acids of formula (I), wherein R.sub.1 and R.sub.2 are hydrogen or C.sub.1 -C.sub.4 alkyl; (A) is hydrogen, halogen, hydroxy or C.sub.1 -C.sub.12 alkyl; (B) is a bond, a C.sub.1 -C.sub.8 alkylene chain, a cycloalkylalkylene chain, an alkylene chain substituted by cyclohexyl or cyclopentyl groups, or an aralkyl chain, an alkyl chain containing an heteroatom (O, S or N--CH.sub.3) or an ureido residue --(CH.sub.2).sub.nl --NHCONH--(CH.sub.2).sub.n --with n ranging from 1 to 5, R.sub.3 is hydrogen, C.sub.1 -C.sub.9 alkyl, C.sub.3 -C.sub.6 cycloalkyl, benzyl, phenyl or p-methoxybenzyl; (C) is C.sub.1 -C.sub.5 alkyl, phenyl or an aralkyl chain; R.sub.4 is hudrogen, C.sub.1 -C.sub.5 alkyl or an amino group optionally substituted by alkyl, phenyl, benzyl, p-methoxybenzyl, acyl, amminoacidic or peptide groups; R.sub.5 and R.sub.6 are 2-haloethyl or together form a 1-aziridinyl residue, are useful as antitumor agent.

Abstract: The invention describes tautomeric compounds of the formula Ia, Ib or Ic ##STR1## and/or their physiologically tolerable salts, in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are a hydrogen atom, substituted (C.sub.1 -C.sub.7)-alkyl, (C.sub.3 -C.sub.10)-cycloalkyl, substituted phenyl or (C.sub.1 -C.sub.4)-alkylphenyl, R.sup.2 is substituted phosphoric acid, R.sup.2 and R.sup.3, R.sup.2 and R.sup.5 or R.sup.4 and R.sup.5 form a monocyclic 5- to 7-membered saturated or unsaturated heterocyclic ring which is mono- or polysubstituted, R.sup.8, R.sup.9, R.sup.10 and R.sup.11 are a hydrogen atom or (C.sub.1 -C.sub.5)-alkyl, X is a hydrogen atom, hydroxyl or halogen, l and n are an integer from 0 to 7, m is an integer from 0 to 2, and the sum of the numbers l, m and n is less than or equal to 10, a process for the preparation of the compounds of the formula Ia, Ib or Ic, pharmaceuticals and their use for the prophylaxis or treatment of osteoporosis.

Abstract: A urethane reaction product, derived from an alkoxylated diorgano phosphorodithioate and an isocyanate, specifically, toluenediisocyanate and hexamethylene diisocyanate, is a multifunctional antiwear and antioxidant additive for lubricants. The isocyanate groups of the reaction product are substantially converted to urethane and/or urea groups through post reaction with active hydrogen compounds such as dibutylamine, bis(2-hydroxethyl) cocoamine and alcohols such as 2-propanol.

Abstract: The present invention relates to a series of novel phospholipid polymers and processes for their use in personal care applications. The compounds of the present invention are prepared by the reaction of a suitable phosphating agent with a pendant hydroxyl group which is present on a polyoxyalkylene polymer, followed by neutralization to a pH of between 6 and 11, followed by the reaction with epichlorohydrin followed lastly by the reaction with a tertiary amine to give a quaternary compound.

Abstract: This compound (I) is prepared by reaction of a compound (II) with carbon disulphide in the presence of an oxidizing agent. It can be used as an agent performing the triple function of initiator, chain transfer agent and termination agent in the radical polymerization of vinyl monomers. The .alpha.,.omega.-difunctional vinyl oligomers and polymers thus obtained are fireproofing polymers or polymers which can be employed as additives in the preparation of fireproofing polymers. They can also be employed to manufacture block polymers by condensation of their end functional groups in the presence of at least one other functional oligomer or polymer, these block polymers also being fireproofing polymers. ##STR1## R.sub.1, R.sub.2 =especially C.sub.1 -C.sub.12 alkyl optionally interrupted by --0--or, ##STR2## cycloalkyl, aryl, --Y--R.sub.4 (Y=single bond, --0-- or --NR.sub.5); R.sub.4 =phosphate or phosphonate functional group; at least one of R.sub.1 and R.sub.

Abstract: 5,5-Bis(perfluoroalkylheteromethyl)-2-hydroxy-2-oxo-1,3,2-dioxaphosphorinan es, derived acyclic phosphorus and phosphoric acids obtained by ring-opening, and salts or esters thereof are prepared from heteroatom containing perfluoroalkyl terminated neopentyl glycols of the formula: HO[CH.sub.2 C(CH.sub.2 --X--E.sub.n --R.sub.f).sub.2 CH.sub.2 O]H by cyclization with appropriate phosphorus containing esters or acids, or hydrolysis. These compositions provide improved thermal stability, and useful low surface energy oil and water repellent coatings for textiles, glass, paper, leather and other materials.Another aspect of this invention relates to the use of the phosphite group containing products as polymer stabilizers.

Abstract: The N-phosphorylation of basic nitrogenous drug compounds to produce pro-drugs with enhanced water solubility or lipid solubility, or reduced toxicity, is disclosed. Drugs containing amine, amidine, guadinine, isourea, isothiourea an biguanide functions may be converted to such pro-drugs. The pro-drugs are hydrolyzed in the body, regenerating the original drugs with the release of a salt of phsophoric acid.

Abstract: Amide compounds useful as additives in lubricating fluids as extreme pressure/antiwear agents are produced on a manufacturing scale. The amides are produced by simultaneously adding together and reacting a phosphorus-containing acid and aqueous acrylamide. Substantially equal molar amounts of the phosphorus-containing acid and the aqueous acrylamide are added together with sufficient cooling to maintain the reaction at a temperature below 50.degree. C. After isolation, the reaction product obtained is preferably further reacted with a coupling agent, preferably paraformaldehyde.

Abstract: Diphosphonate compounds, processes for their preparation and pharmaceutical compositions containing them and being useful for treating calcium metabolism disorders. The diphosphonates are of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen, acyl or alkyl which can be substituted by aryl, R.sub.3 and R.sub.4 are hydrogen or alkyl or R.sub.3 and R.sub.4 together represent lower alkylene, R.sub.5 is a hydrogen atom or alkyl, X is a valency bond or alkylene, Y is a valency bond, alkylene or substituted alkylene, Z is hydrogen, hydroxyl or amino group optionally substituted by alkyl and n is 1, 2 or 3; and including the pharmacologically acceptable salts thereof.

Abstract: A load-carrying agent and a lubricating composition containing such an agent is disclosed. The agent is preferably comprised of a statistical mixture of a plurality of different coupled phosphorus-containing amide compounds having the formula ##STR1## wherein X.sup.1, X.sup.2 and X.sup.3, independently, is O or S; wherein R.sup.1 and R.sup.2, independently, is a hydrocarbyl, a hydrocarbyl-based oxy, the hydrocarbyl portion of which contains 6 to 22 carbon atoms, or a hydrocarbyl-based thio having from 4 to about 34 carbon atoms; wherein R.sup.3, R.sup.4, R.sup.5 and R.sup.6, independently, is hydrogen, or an alkyl having from 1 to about 22 carbon atoms, a cycloalkyl having from about 4 to about 22 carbon atoms, or an aromatic, an alkyl-substituted aromatic or an aromatic-substituted alkyl having from 6 to about 34 carbon atoms; wherein n is 0 or 1; wherein n' is 1, 2 or 3; wherein R.sup.7 is hydrogen or an alkyl having from 1 to 22 carbon atoms; and wherein when n' is 1, R.sup.

Abstract: When applied as safeners, the haloacylaminoalkylphosphinates, haloacylaminoalkylphosphinates and haloacylaminoalkylphosphine oxides of the formula I below are able to protect cultivated plants from the phytotoxic effects of herbicides. Suitable crops are preferably sorghum, cereals, rice, maize and soya beans and the herbicides employed are chloroacetanilides and thiocarbamates.The haloacylaminoalkylphosphonates, haloacylaminoalkylphosphinates and haloacylaminoalkylphosphine oxides have the formula I ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.2 -C.sub.4 alkenyloxy, C.sub.2 -C.sub.4 alkynyloxy, C.sub.1 -C.sub.4 haloalkyl, C.sub.2 -C.sub.8 alkoxyalkoxy or C.sub.1 -C.sub.4 cyanoalkoxy,R.sub.2 is hydrogen or a substituent as defined for R.sub.1,R.sub.3 and R.sub.4 are each independently hydrogen, C.sub.1 -C.sub.4 alkyl or one of R.sub.3 and R.sub.4 is also a radical ##STR2## or both taken together with the carbon atom to which they are attached are also a C.sub.3 -C.sub.