Abstract: Provided herein are processes for preparing an oligomer (e.g., a morpholino oligomer). The synthetic processes described herein may be advantageous to scaling up oligomer synthesis while maintaining overall yield and purity of a synthesized oligomer.

Abstract: Provided herein are processes for preparing an oligomer (e.g., a morpholino oligomer). The synthetic processes described herein may be advantageous to scaling up oligomer synthesis while maintaining overall yield and purity of a synthesized oligomer.

Abstract: Methods for isolating 9-{(R)-2-[((S)-{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine (compound 16): a method for preparing, in high diastereomeric purity, intermediate compounds 13 and 15: and a method for preparing intermediate compound 12: 9-{(R)-2-[((S)-{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine has anti-viral properties.

Abstract: The present invention relates to bisaryl (thio)morpholine derivatives of the formula (I) or a pharmaceutically acceptable salt, a solvate or hydrate thereof, with the proviso that the derivative of formula (I) is not 2-[4-(4-chlorophenoxy)-2-chlorophenyl]-4 -morpholineethanol. The compounds of the invention have affinity to S1 Preceptors and may be used in the treatment, alleviation or prevention of S1 Preceptor mediated diseases and conditions.

Abstract: N2-phosphinyl amidine compounds, N2-phosphinyl amidinates, N2-phosphinyl amidine metal salt complexes, N2-phosphinyl amidinate metal salt complexes are described. Methods for making N2-phosphinyl amidine compounds, N2-phosphinyl amidinates, N2-phosphinyl amidine metal salt complexes, and N2-phosphinyl amidinate metal salt complexes are also disclosed. Catalyst systems utilizing the N2-phosphinyl amidine metal salt complexes and N2-phosphinyl amidinate metal salt complexes are also disclosed along with the use of the N2-phosphinyl amidine compounds, N2-phosphinyl amidinates, N2-phosphinyl amidine metal salt complexes, and N2-phosphinyl amidinate metal salt complexes for the oligomerization and/or polymerization of olefins.

Abstract: The present invention provides a nonaqueous electrolyte solution, which can improve flame retardancy and ameliorate performances of a battery without deteriorating the basic battery performance as far as possible, and a secondary battery. The nonaqueous electrolyte solution is a nonaqueous electrolyte solution for a secondary battery that contains metal salts including ions of metals belonging to group 1 or 2 of the periodic table and a specific cyclic compound having phosphorus and nitrogen atoms in a non-protonic solvent. The non-protonic solvent is a solvent that contains at least one kind of carboxylic acid ester compound and carbonic acid ester compound, and a ratio (MPN/Ms) between a mass (Ms) of the non-protonic solvent containing the metal salts and a mass (MPN) of the cyclic compound is 0.01 to 1.

Abstract: Disclosed is a method for highly efficiently obtaining an optically active alcohol from a carbonyl compound highly enantioselectively. Also disclosed is a ligand used in such a method. Specifically, an optically active alcohol is obtained by reacting a carbonyl compound and an organozinc compound by using a ligand (L) shown below.

Abstract: N2-phosphinyl amidine compounds, N2-phosphinyl amidinates, N2-phosphinyl amidine metal salt complexes, N2-phosphinyl amidinate metal salt complexes are described. Methods for making N2-phosphinyl amidine compounds, N2-phosphinyl amidinates, N2-phosphinyl amidine metal salt complexes, and N2-phosphinyl amidinate metal salt complexes are also disclosed. Catalyst systems utilizing the N2-phosphinyl amidine metal salt complexes and N2-phosphinyl amidinate metal salt complexes are also disclosed along with the use of the N2-phosphinyl amidine compounds, N2-phosphinyl amidinates, N2-phosphinyl amidine metal salt complexes, and N2-phosphinyl amidinate metal salt complexes for the oligomerization and/or polymerization of olefins.

Abstract: Disclosed is a method for highly efficiently obtaining an optically active alcohol from a carbonyl compound highly enantioselectively. Also disclosed is a ligand used in such a method. Specifically, an optically active alcohol is obtained by reacting a carbonyl compound and an organozinc compound by using a ligand (L) shown below.

Abstract: The present invention relates to novel phosphorous derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.

Abstract: The present application provides for a compound of Formula (I) or (II): or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods that include the administration of such compounds with at least one additional active agent.

Abstract: N2-phosphinyl amidine compounds, N2-phosphinyl amidinates, N2-phosphinyl amidine metal salt complexes, N2-phosphinyl amidinate metal salt complexes are described. Methods for making N2-phosphinyl amidine compounds, N2-phosphinyl amidinates, N2-phosphinyl amidine metal salt complexes, and N2-phosphinyl amidinate metal salt complexes are also disclosed. Catalyst systems utilizing the N2-phosphinyl amidine metal salt complexes and N2-phosphinyl amidinate metal salt complexes are also disclosed along with the use of the N2-phosphinyl amidine compounds, N2-phosphinyl amidinates, N2-phosphinyl amidine metal salt complexes, and N2-phosphinyl amidinate metal salt complexes for the oligomerization and/or polymerization of olefins.

Abstract: The present disclosure relates to (thio)morpholine derivatives of the formula (I) wherein R1 is selected from cyano, (2-4C)alkynyl, (1-4C)alkyl, (3-6C)cycloalkyl, (4-6C)cycloalkenyl, (6-8C)bicycloalkyl, (8-10C)bicyclic group, each optionally substituted with (1-4C)alkyl, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, (1-4C)alkyl optionally substituted with one or more fluoro atoms, (2-4C)alkynyl, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino, —SO2-(1-4C)alkyl, —CO-(1-4C)alkyl, —CO—O-(1-4C)alkyl, —NH—CO-(1-4C)alkyl and (3-6C)cycloalkyl, phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl, monocyclic heterocycle optionally substituted with halogen, (1-4C)alkyl or with phenyl optionally substituted with (1-4C)alkyl, and bicyclic heterocycle optionally substituted with (1-4C)alkyl; A is selected from —

Abstract: The present invention relates to ligands and catalyst systems and a process for the simultaneous trimerization and tetramerization of olefinic monomers using said ligands, the ligands having the general formula (I): (R1)2P—P(R1)m(R2)n?N(R3)??(I) wherein R3 is selected from hydrogen, a hydrocarbyl group, a substituted hydrocarbyl group, a heterohydrocarbyl group, a substituted heterohydrocarbyl group, a silyl group or derivative thereof; the R1 groups are independently selected from an optionally substituted aromatic group bearing a polar substituent on at least one of the ortho-positions; and the R2 groups are independently selected from hydrocarbyl, substituted hydrocarbyl, heterohydrocarbyl and substituted heterohydrocarbyl groups with the proviso that when the group is aromatic it does not contain a polar substituent at any of the ortho-positions; with the proviso that m is 0 or 1, n is 1 or 2 and the total of m+n is 2.

Abstract: Disclosed is a method for highly efficiently obtaining an optically active alcohol from a carbonyl compound highly enantioselectively. Also disclosed is a ligand used in such a method. Specifically, an optically active alcohol is obtained by reacting a carbonyl compound and an organozinc compound by using a ligand (L) shown below.

Abstract: The present invention relates to novel phosphorous derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.

Abstract: The invention suggests a pH-sensitive cationic lipid with a pKa value between 3.5 and 8, according to the general formula cation-spacer-Y-spacer-X-lipid, wherein Y and X represent linking groups. Furthermore, liposomes are described, which liposomes include said optionally cationic lipids.

Abstract: Oligonucleotide analogues comprising modified intersubunit linkages and/or modified 3? and/or 5?-end groups are provided. The disclosed compounds are useful for the treatment of diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects.

Abstract: Water soluble reagents and methods for the formation of an amide bond between a phosphinothioester and an azide in an aqueous medium. The phosphinothioester is generated using a water-soluble phosphinothiol reagent. This reaction allows formation of an amide bond between a wide variety of chemical species including amino acids, peptides or protein fragments in an aqueous solution. Of particular interest, this reaction allows for the formation of an amide bond in a physiological setting. In a specific embodiment, this invention provides reagents and methods for peptide ligation in an aqueous medium. The reaction eliminates the need for a cysteine residue and is traceless leaving no residual atoms in the ligated peptide product.

Abstract: An electrostatic-image-developing toner includes a phosphonic acid based sequestering agent.

Abstract: Hypophosphorous acid derivatives having Formula (I) wherein .M is a [C(R3,R4)]n1-C(E,COOR1,N(H,Z)) group, or an optionally substituted Ar—CH(COOR1,N(H,Z)) group, or an a, ?, or a ?, g-cyclic amino acid; .R1 is H or R, R being an hydroxy or a carboxy protecting group; .Z is H or an amino protecting group R?, benzyl oxycarbonyl, benzyl or benzyl substituted; .E is H or a C1-C3 alkyl, aryl, an hydrophobic group; .

Abstract: The present invention relates to ligands and catalyst systems and a process for the simultaneous trimerization and tetramerization of olefinic monomers using said ligands, the ligands having the general formula (I): (R1)2P—P(R1)m(R2)n?N(R3)??(I) wherein R3 is selected from hydrogen, a hydrocarbyl group, a substituted hydrocarbyl group, a heterohydrocarbyl group, a substituted heterohydrocarbyl group, a silyl group or derivative thereof; the R1 groups are independently selected from an optionally substituted aromatic group bearing a polar substituent on at least one of the ortho-positions; and the R2 groups are independently selected from hydrocarbyl, substituted hydrocarbyl, heterohydrocarbyl and substituted heterohydrocarbyl groups with the proviso that when the group is aromatic it does not contain a polar substituent at any of the ortho-positions; with the proviso that m is 0 or 1, n is 1 or 2 and the total of m+n is 2.

Abstract: The present invention relates to compositions useful for treating or controlling disease states or conditions associated with zinc containing proteinases, especially metalloproteinases. The active ingredient in these compositions is an alpha-oxo- or alpha-thioxophosphonate of formula (I). Out of the phosphonates of formula (I), some are known and others are new. The novel compounds constitute another aspect of the invention.

Abstract: Novel compounds of the formula (I), in which R1, R2, R3, X and Y have the meaning indicated in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumors.

Abstract: The invention provides novel pyrophosphate synthase inhibitors of formula I as well as compositions comprising such inhibitors and methods for their use.

Abstract: The invention is a water treatment composition comprising at least one phosphonamide and blends thereof and a method to treat water. As phosphonamides are generally odorless, and typically solids, phosphonamide and phosphonamide blend compositions are generally odorless, conveniently processed and manufactured, and safely used without risks of exposure to odors and vapors associated with the corresponding amines. Advantageously, phosphonamides blended with amino-phosphate esters provide useful treatment compositions. The inventive compositions are generally used to treat water contained in water flow systems such as boilers and cooling towers.

Abstract: The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.

Abstract: The present invention relates to nitroaryl-substituted phosphoramide prodrug compounds and methods of producing the same for use in targeting and inhibiting undesirable cell growth or proliferation.

Abstract: This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.

Abstract: Novel styrylacrylonitrile compounds which are useful in treating a variety of cell proliferative disorders such as cancer are disclosed.

Abstract: The present application describes novel cyclic &bgr;-amino acid derivatives of formula I: 1

Abstract: The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which R1, R2, R3 and A are each as defined, and to processes for their preparation and to their use as medicaments, in particular as medicaments for the treatment of cardiovascular disorders.

Abstract: A compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof: wherein R1 represents hydrogen atom, an alkyl group, a substituted alkyl group and the like; R2 and R3 represent hydrogen atom, an alkyl group, a substituted alkyl group, an alkoxyl group and the like; X represents —CH2—, —O—, or —NH—; A represents the following group (II): [in which R7 and R8 represent hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group and the like; R9 and R10 represents hydrogen atom, a halogen atom, hydroxyl group, phenyl group, an alkyl group and the like] and the like; and E represents hydrogen atom and the like, which has inhibitory activity against carboxypeptidase B and is useful for therapeutic and/or preventive treatment of a thrombotic disease.

Abstract: The present invention relates to compounds of the formula 1

Abstract: The invention relates to a prodrug that is capable of being converted into a drug by the catalytic action of human fibroblast activation protein (FAP&agr;), said prodrug is chemically stable under physiological conditions and can be used for the manufacture of physically stable aqueous formulations. It has a cleavage site which is recognised by FAP&agr;, and the drug released by the enzymatic activity of FAP&agr; is cytotoxic or cytostatic under physiological conditions.

Abstract: The present application describes novel cyclic hydroxamic acids of formula I: 1

Abstract: The present application describes novel lactams and derivatives thereof of formula I: 1

Abstract: This invention features conjugates, degradable linkers, compositions, methods of synthesis, and applications thereof, including galactose, galactosamine, N-acetyl galactosamine, PEG, phospholipid, peptide and human serum albumin (HSA) derived conjugates of biologically active compounds, including antibodies, antivirals, chemotherapeutics, peptides, proteins, hormones, nucleosides, nucleotides, non-nucleosides, and nucleic acids including enzymatic nucleic acids, DNAzymes, allozymes, antisense, dsRNA, siRNA, triplex oligonucleotides, 2,5-A chimeras, decoys and aptamers.

Abstract: The present invention relates to polyphosphate ester morpholides, compositions comprising mixtures thereof and thermoplastic resin compositions containing the polyphosphate ester morpholide composition as a flame retardant. The flame retardant compositions comprise mixtures of polyphosphate ester morpholides which are represented by the following general formula I: in which X is 1 or 2; R1 is a C6-C20 aryl group, an alkyl substituted C6-C20 aryl group or a derivative thereof; R2 is a C6-C30 arylene group, an alkyl substituted C6-C30 arylene group or a derivative thereof; n is the average number of morpholide repeating units, m is the average number of R1 repeating units, and n+m is 1 to 5. In accordance with the present invention, it is possible to provide a flame retardant thermoplastic resin compositions having improved flame retardancy even when small amounts of the flame retardant are used.

Abstract: The present invention relates to novel classes of compounds of formula I which are caspase and TNF-alpha inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase and TNF-alpha activity and consequently, can be advantageously used as agents against caspase-, interleukin-1-(“IL-1”), apoptosis-, interferon-&ggr; inducing factor- (IGIF), interferon-&ggr;- (“IFN-&ggr;”), or TNF-alpha mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to processes for preparing the compounds of this invention.

Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.

Abstract: The present invention relates to a compound with aryl-amidines, particularly amidinoaryl-cyclopropanes, amidinoarylmethyl-pyrroles, amidinoaryl-benzenes, amidinoaryl-pyridines, or amindonoaryl-alanines, represented by formula (1), a pharmaceutically acceptable salt, a prodrug, a hydrate, a solvate or an isomer thereof, which are inhibitors of coagulation enzyme, factor Xa (FXa). The present invention also relates to a pharmaceutical composition containing the compound, and a method of using the same as an anticoagulant agent for treatment and prevention of thrombosis disorders.

Abstract: Disclosed is a phenyl boronic acid compound represented by Structural Formula (I): 1

Abstract: The invention relates to the preparation and use as catalysts of diphosphines of the formula (I) 1

Abstract: The present application describes novel amides and derivatives thereof of formula 1

Abstract: Novel cyclo azaphospha hydrocarbons according to formula I 1

Abstract: The disclosed invention is a composition agonists and/or antagonists of V2, V1a or both receptors, in a host, including animals, and especially humans, using a small molecule or its pharmaceutically acceptable salt or prodrug.

Abstract: The present invention describes novel halogenated triphenylethylene derivatives, or pharmaceutically acceptable prodrug or salt forms thereof, as selective estrogen receptor modulators for the treatment of and/or prevention of breast, uterine, ovarian, prostrate and colon cancer, osteoporosis, cardiovascular disease, and benign proliferative disorders, as well as methods for making the compounds and pharmaceutical compositions of this invention.

Abstract: This invention pertains to novel salt forms of trophenylethylene compound, such as 3-[4(1,2-diphenyl-but-1-enyl)-phenyl]-acrylic acid, as selective estrogen receptor modulators. This invention also provides methods for the treatment and/or prevention of breast, uterine, ovarian, prostrate and colon cancer, osteoporosis, cardiovascular disease, and benign proliferative disorders, as well as pharmaceutical compositions of the compounds of the present invention.

Abstract: The invention concerns compositions for manufacturing composite materials containing a polyaniline. These compositions are formed by a solution in a solvent such as m-cresol of the following constituents: a) a conductive polyaniline protonated by means of a protonation agent able to promote the dissolution of the polyaniline in the solvent, for example phenylphosphonic acid, b) an insulating polymer chosen for example from amongst the cellulosic polymers and polyvinyl chlorides such as cellulose acetate, and c) an insulating plasticiser such as a mixture of dimethyl phthalate, diethyl phthalate and triphenyl phosphate. By pouring this solution and evaporating the solvent, it is possible to obtain a flexible film of conductive composite material having good electrical and mechanical properties.