Abstract: A process for the preparation of (S)-N,N?-bis[2-hydroxy-1-(hydroxymethyl)ethyl]-5-[(2-hydroxy-1-oxo-propyl)amino]-2,4,6-triiodo-1,3-benzendicarboxamide (iopamidol) starting from 5-amino-N,N?-bis[2-hydroxy-1-(hydroxymethyl)ethyl]-2,4,6-triiodo-1,3-benzenedicarboxamide (II) which process comprises a) reacting the compound of formula (II) with a suitable protecting agent, to give a compound of formula (III) wherein R is a group of formula A or B wherein R1 is a hydrogen atom, a C1÷C4 straight or branched alkoxy group, R2 is hydrogen, a C1÷C4 straight or branched alkoxy group and R3 ?is a C1÷C4 straight or branched alkyl group, a trifuoromethyl or a trichloromethyl group; b) acylating the amino group in position 5 of the intermediate compound of formula (III), by reaction with a (S)-2-(acetyloxy)propanoyl chloride to give a compound of formula (IV) wherein R is as defined above; and c) removing all the acyl groups present in the compound of formula (IV) under basic conditions, with prior cleavage of the cyclic pr

Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.

Abstract: A group of benzamide compounds are disclosed which are useful for treating neurodegenerative disorders. Methods for making these compounds are provided. These materials are formed into pharmaceutical compositions for oral or intravenous administration to patients suffering from conditions such as Parkinson's disease which can exhibit themselves as progressive loss of central nervous system function. The compounds can arrest or slow the progressive loss of function.

Abstract: The present invention relates to synthetic cationic lipids, liposome formulations and the use of such compounds to introduce functional bioactive agents into cultured cells.

Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.

Abstract: Conformationally restricted polyamine compounds useful in treatment of cancer and other diseases marked by abnormal cell proliferation are disclosed. Improved methods of synthesizing such compounds are also disclosed. In one method of the invention, a carbene-bearing or carbene equivalent-bearing compound is reacted with the double bond of an alkene compound to form a cyclopropyl ring as the first step in the synthesis.

Abstract: A process for the preparation of iodixanol by dimerization of 5-acetamido-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-isophthalamide (“Compound A”) in which, after the dimerization step, unreacted Compound A is precipitated from the reaction mixture and recovered for re-use. The process substantially increases the net yield of iodixanol and simplifies its purification.

Abstract: The present invention provides basic ionic contrast agents that have anticoagulant activity. The contrast media incorporate a lysine or arginine group or derivative, and have a free amino or guanidino group. Methods of using the contrast media are also disclosed.

Abstract: The present invention provides a basic amino acid derivative represented by the formula (1): The present invention also provides a method of making a gelled product by employing the aforementioned compound, as well as a gel, perfumery, and/or cosmetic containing the same.

Abstract: The invention relates to the use of compounds (A) with at least one structural unit of formula (I), wherein X represents groups of formula —CR1?CR2— or a carbonyl group C?O, R1 and R2 meaning hydrogen or essentially organic radicals, Z means essentially organic radicals, n means a number from 0 to 3 and p means a number from 0 to 5, as UV absorbers with an affinity for textile fibres, for protecting the human skin from harmful UV radiation and for protecting dyed textile materials from fading.

Abstract: This invention relates to compounds of formula (I)

Abstract: The invention relates to bisaryl derivatives of the formula I, wherein (R,R) is selected from (H,H), O, (H,CH3), (H,OH) and (H,CN); Ar is substituted phenyl and A is a group of formula II, III, IV or V: An example is (3S,6S)-1-N-(7-phenylheptyl)-3-(4-(3,4,5-trimethoxyphenyl)benzyl)-4-N-methyl-6-methyl-2,5-dioxo-1,4-piperazine: The compounds of the invention have FSH receptor modulatory activity and can be used for the control of fertility, for contraception or for treatment of hormone-dependent disorders.

Abstract: Purification process of iohexol comprising the treatment of said product with 1-methoxy-2-propanol either alone or mixed with other solvents.

Abstract: The present invention provides a method for preparing dimer of a monohydroxy aromatic compound. In the method of the present invention, oxidative coupling reaction of a monohydroxy aromatic compound represented by formula [I]: Ar—OH??[I] wherein Ar represents an optionally substituted aromatic group is carried out in a nitrogen containing polar solvent in the presence of a copper salt. By the method of the instant invention, dimer of the monohydroxy aromatic compound can be obtained in high yield.

Abstract: A compound and salts and enantiomers thereof, having the formula: wherein R7 is an acyl group.

Abstract: The invention features compounds that inhibit secretion of a protein encoded by an ARE-mRNA or that modulate regulation of an ARE-mRNA. These compounds are useful for the treatment or prevention of conditions involving proteins encoded by ARE-mRNAs, such as TNF?.

Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.

Abstract: Disclosed are compounds which inhibit ?-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits ?-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

Abstract: The present invention provides a binaphthol compound represented by formula [1]: and a salt thereof. The binaphthol compound of the present invention is useful for manufacturing antiseptic compounds or chiral catalysts. According to the method of the present invention, binaphthol compounds can be prepared in high yield with low cost.

Abstract: A drug complex useful as a DDS compound, which is represented by the following formula: A-R—NH—Y—CH2—O—CO-Q, wherein A is a polymer as a drug carrier; R is a spacer, wherein the spacer is an amino acid or an oligopeptide comprising 2 to 8 amino acids; Y is phenylene group which may be substituted; and Q is a residue of a drug compound such as antineoplastic agents. The complex provides rapid and site-selective release of a drug compound such as antineoplastic or anti-inflammatory agents and surely exhibits expected efficacy.

Abstract: The present invention provides compounds having formula (I): 1

Abstract: Novel compounds of the formula (I) in which R1, R2, R3, R4, X and Z are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders and for the treatment of tumours.

Abstract: Peptidomimetic compositions for selective inhibition of neuronal nitric oxide synthase.

Abstract: The present invention discloses a process for the preparation of pure non-ionic contrast agents. The invention also includes a method for purifying the non-ionic contrast agents.

Abstract: The present invention is directed to polymeric prodrug transport forms and methods of making and using the same. In one preferred aspect, the prodrugs are of the formula: wherein G is a polymeric residue; Z is one of: and B is a residue of a biologically active amine-containing moiety or a hydroxyl-containing moiety.

Abstract: Amide, sulfonamide and urea compounds having an inhibitory effect on Src kinase including enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates of said compound, said compound having the general structure shown in Formulae I and II:

Abstract: Compositions of matter and methods for enhancing bioassay performance are disclosed. More particularly, the composition of matter comprises a molecularly compact polymer-ligand conjugate capable of self-orienting on a surface to improve the orientation of the ligand/receptor binding domains within the bioassay at the nanoscopic level. In a preferred embodiment, the molecularly compact polymer comprises a dendrimer polymer such as a fifth generation polyamidoamine dendrimer having exterior surface hydroxyl and amine functional groups, and the ligand/receptor comprises an antibody or Fab.

Abstract: The present invention describes compounds of the general formula I 1

Abstract: Gamma-secretase inhibitors, useful in the treatment or prevention of Alzheimer's disease, are disclosed. The preferred compounds have, as the central portion of the molecule, the structure (a) and are di-astereoisomers of known protease inhibitors.

Abstract: Purification process of iohexol comprising the treatment of said product with 1-methoxy-2-propanol either alone or mixed with other solvents.

Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, &bgr;-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII): useful in treating Alzheimer's disease and other similar diseases.

Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.

Abstract: The invention concerns polyalkoxylated superamides of the following formulae: [R1—CONR2—CH2CHR3—O—CHR4—CHR5O)m—(CH2CH2O)n]9 p(I); R1—CON—[CH2CHR3—O—(CHR4—CHR5O)m—(CH2CH2O)n—X]2, formulae wherein: R1 presents a C7-C22 hydrocarbon radical; R2, R3, represent a hydrogen or a C1-C4 hydrocarbon radical; R4, R5 represent a hydrogen or an alkyl radical comprising 1 to 2 carbon atoms, provided that one or more of said two radicals is a hydrogen; X represents a hydrogen, a C1-C6 hydrocarbon radical, a phosphate, carboxylate, sulphate, sulphonate group; m ranges between 0 and 20 exclusive; n ranges between 0 and 50 exclusive; p is equal to 1 or 2, depending on what X represents. The invention also conerns a method for obtaining said compounds and their use in particular as emulsifying agent for oils.

Abstract: The invention relates to a method for the separation of oligomeric N-substituted (meth)acrylamides and conjugates thereof (enzyme conjugates, affinity macroligands and AML complexes) which are reversibly thermally precipitating from aqueous solutions, whereby the oligomeric N-substituted (meth)acrylamides and conjugates thereof are precipitated thermally and filtered in the presence of salts and filtration adjuncts. The oligomeric N-substituted (meth)acrylamides and conjugates thereof are characterised by a separation rate of over 90% of the thermal precipitate and thus permit an efficient biocatalysis and affinity preparation based on oligomeric compounds which are reversibly thermally precipitating on a large scale.

Abstract: This invention relates to an ocular tension depressor containing a specific benzamide derivative as an active ingredient.

Abstract: Substituted polycarboxylic ligand molecules and corresponding metal complexes of said ligands, preferably paramagnetic metals complexes for generating responses in the field of magnetic resonance imaging (MRI) The paramagnetic complexes of the polycarboxylic ligands possess advantageous tensioactive properties and are useful as MRI contrast media in formulations for investigating the blood pool.

Abstract: A amidoamine composition containing oligomeric amidoamine compounds having the structure: the average of x based on the amidoamine composition is at least 0.2, and Z is the residue of a polyoxyalkylene polyether polycarboxylic acid compound, and the amidoamine composition is the reaction product of primary polyamine compounds with polyoxyalkylene polyether polycarboxylic acid compounds at a corresponding equivalent weight ratio of at least 4.0:1 under oligomeric reaction conditions effective to increase the amine nitrogen equivalent weight of the amidoamine composition by at least 10% over the average acid equivalent weight of said polyoxyalkylene polyether polyacid composition. There is also provided glycidated amidoamine compositions used as epoxy functional surfactants, and the aqueous epoxy resin dispersions thereof, and the curable epoxy resin compositions thereof.

Abstract: The present invention provides compositions and methods to facilitate the identification of compounds that are capable of interacting with a biological macromolecule of interest. In one aspect, a composition is provided that comprises an array of one or more types of chemical compounds attached to a solid support, wherein the density of the array of compounds is at least 1000 spots per cm2. In particularly preferred embodiments, these compounds are attached to the solid support through a covalent interaction.

Abstract: Compounds of formula I, in which R1, R2, A, and B having the definitions set forth in the claims, are valuable pharmacologically active compounds, which exhibit a strong antithrombotic effect and are suitable, for example, for treating thromboembolic diseases and restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. Also disclosed are processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Abstract: The present invention provides novel amide-based cationic lipids of the general structure: or a salt, or solvate, or enantiomers thereof wherein; (a) Y is a direct link or an alkylene of 1 to about 20 carbon atoms; (b) R1 is H or a lipophilic moiety; (c) R2, R3, and R4 are positively charged moieties, or at least one but not all of R2, R3, or R4 is a positive moiety and the remaining are independently selected from H, an alkyl moiety of 1 to about 6 carbon atoms, or a heterocyclic moiety of about 5 to about 10 carbon atoms; (d) n and p are independently selected integers from 0 to 8, such that the sum of n and o is from 1 to 16; (e) X− is an anion or polyanion and (f) m is an integer from 0 to a number equivalent to the positive charge(s) present on the lipid; provided that if Y is a direct link and the sum of n and p is 1 then one of either R3 or R4 must have an alkyl moiety of at least 10 carbon atoms.

Abstract: This invention relates to derivatives of alpha-amino acid amides, to pharmaceutical compositions containing such compounds, and to their use in medicine as inhibitors of cysteine proteases, particularly the cathepsins. A compound of formula (I) is described or a pharmaceutically acceptable salt, hydrate or solvate thereof. Pharmaceutically acceptable salts of the compounds of this invention include the sodium, potassium, magnesium, calcium, hydrogen chloride, tartaric acid, succinic acid, fumaric acid and p-toluenesulfonic acid salts.

Abstract: Process for the preparation of contrast agents The invention provides a process for the preparation of an N-alkyl-acylamino-phenyl-carboxylic acid or carboxylic acid derivative by liquid phase acylation and subsequent N-alkylation of a corresponding amino-phenyl-carboxylic acid (or carboxylic acid derivative), the improvement comprising the addition of an alkylating agent to a solution containing the reaction products of said acylation, to effect said N-alkylation.

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: Compounds of Formula I, and pharmaceutical compositions containing these compounds, activate the insulin receptor kinase, which leads to an increased sensitivity to insulin and an increase in glucose uptake, and are therefore useful for the treatment of animals, especially humans, with hyperglycemia, especially for the treatment of type 2 diabetes. Processes for preparation of the compounds, and their use in assays, are also disclosed.

Abstract: The present invention discloses a new process for producing ioversol (marketed as OPTIRAY®) comprising: (a) reacting 5-amino-N,N′-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisopthalamide with chloroacetyl chloride in a polar aprotic solvent or combinations thereof to produce N,N′-bis[2,3-di(2-chloroacetoxy)propyl]-5-(2-chloroacetamido)-2,4,6-triiodoisophthalamide; (b) reacting the product of (a) with a base to produce N,N′-bis(2,3-dihydroxypropyl)-5-(2-chloroacetamido)-2,4,6-triiodoisopthalamide; (c) reacting the product of (b) with an alkylating agent capable of producing a hydroxyethylated product in the presence of a base and water to produce N,N′-bis(2,3-dihydroxypropyl)-5-[N-(2-hydroxyethyl) (2-chloroacetamido)]-2,4,6-triiodoisopthalamide; and (d) reacting the product of (c) in water and acetate ions to produce ioversol.

Abstract: The object of the present invention is to provide ethylamine derivatives that function as a motilin receptor antagonist and that are useful as medicines. The invention provides compounds represented by the general formula (1): wherein R1 represents a phenyl group or the like, R2 represents a hydrogen atom and the like, R3 represents a hydrogen atom and the like, R4 represents a hydrogen atom and the like, R5 represents an alkyl group and the like, R7 represents a hydrogen atom and the like and R8 represents a heterocyclic ring and the like; or a hydrate or pharmaceutically acceptable salt thereof and a medicine which comprises the above compound or a hydrate or pharmaceutically acceptable salt thereof as an active ingredient.

Abstract: A labeling reagent for use in oligonucleotide (“oligo”) synthesis, as well as a method of preparing such a labeling reagent, a method of using such a reagent for synthesizing a labeled oligonucleotide, and an oligonucleotide prepared using such a reagent. The reagent can be used to label either the 3′ or 5′ termini of a synthesized oligo, and/or for one or more positions along the oligo. The labeling reagent can be prepared by a reaction scheme that involves the initial preparation of hydroxyacids, tritylated hydroxyacids and coupling of such derivatives to diamine, wherein the amine function serves at an attachment point for labels and the hydroxyl groups can either be used to immoblize the molecules to support or can be converted to provide a phosphorylating reagent.

Abstract: This invention provides a novel class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds which are tissue-selective androgen receptor modulators (SARM), which are useful for oral testosterone replacement therapy, male contraception, maintaining sexual desire in women, treating prostate cancer and imaging prostate cancer. These agents have an unexpected in-vivo activity for an androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. These agents may be active alone or in combination with progestins or estrogens. The invention further provides a novel class of non-steroidal agonist compounds. The invention further provides compositions containing the selective androgen modulator compounds or the non-steroidal agonist compounds and methods of binding an androgen receptor, modulating spermatogenesis, treating and imaging prostate cancer, and providing hormonal therapy for androgen-dependent conditions.

Abstract: The present invention is directed to a process for the preparation of a compound of formula (X-a) or a pharmaceutically acceptable salt form thereof, wherein: R1 is selected from the group consisting of: C1-5 alkyl substituted with 0-5 R1a, —(CH2)r—C3-10 cycloalkyl substituted with 0-5 R1a, and —(CH2)r-aryl substituted with 0-5 R1a. Compounds of Formula (X-a) are macrocyclic molecules containing anti-succinate residues which inhibit metalloproteinases such as aggrecanase, and the production of tumor necrosis factor (TNF). The anti-succinates are formed by an Ireland Claisen rearrangement of a silyl ketene acetal which proceeds with high stereoselectivity.