Abstract: The present invention is drawn to novel antiviral compounds, pharmaceutical compositions and their use. More specifically this invention is drawn to derivatives of monocyclic polyamines which have activity in standard tests against HIV-infected cells as well as other biological activity related to binding of ligands to chemokine receptors that mediate a number of mammalian embryonic developmental processes.

Abstract: The subject invention pertains to macrocyclic compounds, and their use, the compounds having the formula (I) 1

Abstract: Expanded porphyrin comprising substitutions for at least two NH groups by S, Se or Te are non-photoactive and are selective for binding G-quadruplexes characteristic of the c-MYC control region. Accordingly, these expanded porphyrins are useful to modulate the expression of genes controlled by the formation of c-MYC type G-quadruplexes, such as c-MYC itself.

Abstract: The present invention relates to charge transport compositions. The invention further relates to electronic devices in which there is at least one active layer comprising such charge transport compositions.

Abstract: The instant invention relates to stable free nitroxyl radicals of formula (I) at least one of the substituents R is —O. and the others are hydrogen or OH; X is —NR1R2, wherein R1 and R2 are independently hydrogen, C1-C18alkyl or together with the nitrogen atom to which they are bound from a 5 or 6 membered ring which may be further interrupted by an O atom. Further subjects of the invention are an oxidation process for alcohols to aldehydes or ketones or to carboxylic acids in the presence of a compound of formula (I) and the use of stable free nitroxyl radicals of formula (I) as oxidation catalysts.

Abstract: A method of manufacturing substance GM-95 having general formula [I], comprising (a) deprotecting a macrocyclic compound having general formula [II] (wherein, R1's are the same or different and each represents a lower alkyl group, and R2 represents a thiol protecting group) by removing acetal protecting groups (the R1's) thereof, and forming an oxazole ring through an intramolecular cyclization reaction between produced formyl group and an amide group, and (b) deprotecting a resulting macrocyclic compound having general formula [III] (wherein, R2 is as mentioned above) by removing the thiol protecting group (R2) thereof, and forming a thiazoline ring through an intramolecular cyclization reaction between a thiol group thus produced and an amide group.

Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6, R7, R8, R9, X, b, k, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.

Abstract: Cucurbituril derivatives, their prepartion methods and uses.

Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided: 1

Abstract: A series of N,N′-dimethylated N-confused porphyrin salts were synthesized through methylation of N-confused porphyrins using MeI in the presence of Na2CO3. These compounds have an intense absorption around 790 nm. It has also been shown that N,N′-dimethylated N-confused porphyrin salts can generate singlet oxygen when irradiated. They are, thus, potential sensitizers for PDT.

Abstract: Methods of modifying polypyrrolic macrocycles by use of a 1,3-dipolar cycloaddition is described. The methods may be used to produce compounds for further derivatization to produce photosensitizing agents of interest.

Abstract: Disclosed are the general principles upon which closed molecular or ionic structural frameworks may be prepared. These frameworks are based upon the self-assembly (wherein the term self-assembly refers to the association of chemical components through inter-component bonds) of n>4 subunits where surface curvature is supplied by edge sharing of subunits.

Abstract: The present invention provides an oxidative coupling procedure that allows efficient synthesis of novel cyclo[n]pyrrole macrocycles. Therefore, the present invention provides cyclo[n]pyrroles where n is 6, 7, 8, 9, 10, 11, or 12, and derivatives, multimers, isomers, and ion and neutral molecule complexes thereof as new compositions of matter. A protonated form of cyclo[n]pyrrole displays a gap of up to 700 nm between strong Soret and Q-like absorption bands in the electronic spectrum, demonstrating no significant ground state absorption in the visible portion of the electronic spectrum. Uses of cyclo[n]pyrroles as separation media, nonlinear optical materials, information storage media and infrared filters are provided.

Abstract: The present invention provides a process of synthesizing a compound of Formula I by treating, in an inert medium and in the presence of an organic base, a compound of formula A with an organo metallic agent capable of acting as an outer sphere oxidant to form a compound of Formula I.

Abstract: Novel derivatives of metallotexaphyrins are prepared by modifying the apical ligands associated with the central metal component of a metallotexaphyrin.

Abstract: A compound which has the following formula (1), 1

Abstract: Novel compounds that either preferentially absorb into hyperproliferative tissue and absorb light efficiently at a wavelength of between about 700 and about 850 nm or act as intermediates for such absorbing compounds.

Abstract: A compound which has the following formula (1), a process for its production, a pharmaceutical composition comprising the compound as an active ingredient, a method of treating tumor which comprises administering the compound, use of the compound as a medicine, and a microorganism capable of producing the compound. The compound of the present invention is a novel compound which has antitumor action and is useful as a medicine.

Abstract: A formulation and method for therapeutic treatment of in mammals using certain metals or particle-emitting radionuclides complexed with tetraazamacrocyclic ligands are described.

Abstract: The present invention is directed to piperazine-containing macrocyclic compounds which inhibit prenylyl-protein transferase, such as farnesyl-protein transferase (FTase), and therefore inhibit the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

Abstract: Polyamines containing at least two nitrogen atoms monosubstituted with pendant arms capable of coordinating metal cations, or with precursors of such pendant arms, all nitrogen atoms of the polyamines except two being fully substituted and the remaining two bearing one H atom each, are cyclized by reaction with a bridging agent that contains two sites that each bear a reactive group capable of undergoing a nucleophilic attack by one of the two N-H groups on the polyamine. Unlike the prior art, cyclization occurs in preference over polymerization of the polyamine, even in reaction mixtures in which the polyamine is at high concentration. A process is also disclosed whereby linear polyamines in which the terminal amine groups are primary amines are substituted with methylenephosphonate ester groups, with one such substituent on each nitrogen atom of the polyamine.

Abstract: A method of making chlorins comprises the steps of reacting (e.g. condensing) a dipyrrin western half intermediate with an eastern half intermediate to form a tetrahydrobilene, and then cyclizing the tetrahydrobilene to form a chlorin. Intermediates including tetrahydrobilenes useful in such reactions are also described.

Abstract: There is provided compounds of formula I, wherein R1, R2, R3, R4, R41 to R46, A, B and G have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.

Abstract: Novel macrocyclic compounds are constructed to include large cyclic structures that are interrupted by at least one ring system. Each interrupting ring system includes two bridgehead atoms. Bridgehead atoms are bonded to one or more bridges that interconnect one or more ring systems thereby forming a large cyclic structure. Located in each bridge are two or more nitrogenous moieties that are derivatized with chemical functional groups. The ring systems can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring. These can also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the macrocyclic compounds. In accordance with certain embodiments of the invention, libraries of such macrocyclic compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the library.

Abstract: The present invention relates to a process for preparing a cross-bridged tetraaza macrocyclic ligands having formula (I), wherein each R is independently C1-C22 linear alkyl, C1-C22 branched alkyl, C7-C22 alkylenearyl, C8-C22 alkyl substituted alkylenearyl, and mixtures thereof; each index n is independently from 0 to 3, by contacting the a di-quaternary cis tetracycle precursor with as little as one equivalent of a borohydride reducing agent. The present process eliminates the need to use up to a twenty fold excess of reducing agent thereby further eliminating the need for work-up conditions which liberate significant amounts of hydrogen gas and which requires the disposal of large amounts of boron waste products.

Abstract: This invention is directed to macroheterocyclic compounds useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.

Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.

Abstract: The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

Abstract: The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

Abstract: Disclosed are compounds which are conjugates of (a) a moiety capable of localizing in the cells of a tumor or atheroma and (b) a moiety capable of catalyzing the production of reactive oxygen species from a cellular metabolite. The disclosed compounds which are useful for treating atheroma, tumors and other neoplastic tissue.

Abstract: The present invention is drawn to novel antiviral compounds, pharmaceutical compositions and their use. More specifically this invention is drawn to derivatives of monocyclic polyamines which have activity in standard tests against HIV-infected cells as well as other biological activity related to binding of ligands to chemokine receptors that mediate a number of mammalian embryonic developmental processes.

Abstract: This invention involves synthesis and use of a class of compounds with chelation affinity and selectivity for first transition series elements. Administration of the free or conjugated compound, or physiological salts of the free or conjugated compound, results in decrease in the in vivo bioavailability of first transition series elements and/or removal from the body of first transition series elements and elements with similar chemical properties. These characteristics make such compounds useful in the management of diseases associated with a bodily excess of first transition series elements and elements with similar chemical properties. This invention demonstrates that such compounds inhibit mammalian, bacterial, and fungal cell replication and are therefore useful in the treatment of neoplasia, infection, inflammation, immune reponse, and in termination of pregnancy.

Abstract: Cucurbituril derivatives, their prepartion methods and uses.

Abstract: This invention relates to novel potassium channel blocking agents, and their use in the preparation of pharmaceutical compositions.

Abstract: The invention disclosed herein involves a phototherapeutic pyrrolic core complexed with a non-radioactive Indium atom. Complexation of Indium by the pyrrolic core forms a metalopyrrolic compound which influences enables these compounds to localize at target sites a phototherapy. Such functionally aids in both detection and phototherapy of disease sites, or provides functionality that binds to site specific receptors of a target area such that the therapy is improved.

Abstract: Improved synthesis of a macropolycycle, more particularly, of a cross-bridged tetraazamacrocycle.

Abstract: The present invention is directed to macrocyclic compounds which inhibit prenyl-protein transferase (FTase) and the prenylation of the oncogene protein Ras. The invention is further directed to chemothera-peutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

Abstract: The present invention provides halogenated calixpyrrole, calixpyridinopyrrole, and calixpyridine macrocycles having 4-12 pyrrolic rings with greater stability, enhanced anion and neutral molecule binding affinity, and different binding selectivites as compared to their nonhalogenated congeners as judged from 1H NMR, 19F NMR and fluorescence emission spectroscopic analyses.

Abstract: 1,4,7,10-tetraazacyclododecane-1,4-diacetic acid of formula (I): as well as its chelated complex salts with bi-valent metal ions having atomic numbers from 20 to 31, 39, 42, 43, 44, 49, or from 57 to 83, as well as their salts with anions of physiologically acceptable organic acid selected from acetate, succinate, citrate, fumarate, maleate, oxalate, or with anions of inorganic acids selected from halo acids ions. The compounds are intermediates for preparing 1,4,7,10-tetraaza-cyclododecane chelating agents.

Abstract: The present invention is directed to peptidomimetic macrocyclic compounds of the formula A: wherein W is a heterocycle, V is a heterocycle or aryl moiety and Z1 is a suitably substituted aryl or heterocycle moiety. The instant compounds inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

Abstract: The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

Abstract: A novel class of macrocycles, termed triazatrinaphthyrins, is disclosed having general Formula I: 1

Abstract: A novel class of macrocycles, termed triazatrinaphthyrins, is disclosed having general Formula I: or a solvate, hydrate, ester or salt thereof; wherein R1, R2, R3, Ra, Ra′, Ra″, Rb, Rb′, Rb″, Rc, Rc′, Rc″, Rd, Rd′ and Rd″ are defined in the specification. The macrocycles are useful in the extraction of transition metals, in particular in the extraction of lanthanides.

Abstract: The invention relates to novel magnetic resonance imaging contrast agents.

Abstract: Cyclic bis benzimidazole ligands of the following formula are formed by contacting a (2-aminophenyl)-benzimidazole-4-carboxaldehyde ethylene acetal or a (2-nitrophenyl)-benzimidazole-4-benzaldehyde with an acid optionally in the presence of a metal or a metal salt. wherein R1 and R2 may be the same or different and are selected from H, an alkyl having 1 to 10 carbon atoms, a benzyl group, a substituted 2-ethylphenyl group, a carbonyl group, a phenyl substituent, a tosyl group, and an alkylsulfonate group; R3 and R4 may be the same or different and are selected from H, methyl, and ethyl; and R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, and R18 may be the same or different and are selected from H, alkyl having 1 to 10 carbon atoms, fluoride, chloride, bromide, iodide, nitro, amino, a carboxylate, an ester, and a phenyl group.

Abstract: The present invention relates to novel heteroaryl diazabicycloalkane derivatives represented by general formula (I), any of its enantiomers or any mixture thereof, an N oxide thereof, a pharmaceutically acceptable salt thereof, in a labelled or un-labelled form, which are found to be cholinergic ligands at the nicotinic Acetyl Choline Receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neurodegeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.

Abstract: The present invention is directed to novel fused aryl and heteroaryl bridged indenopyrrolocarbazoles which are useful, inter alia, as therapeutic agents. The invention is also directed to methods for making and using the bridged indenopyrrolocarbazoles.

Abstract: The present invention is directed to macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

Abstract: Compounds of formula (I) in which R is in which R is hydrogen, a straight or branched or cyclic C1-C6 alkyl group, unsubstituted or substituted by 1 to 10 oxygen atoms, or a C1-C20 alkyl group, optionally interrupted by a phenylene, in turn substituted by a straight or branched C1-C6 alkyl group, unsubstituted or substituted by 1 to 3 C1-C7 alkyl groups; the phenylene group being unsubstituted or substituted by alkoxy, carboxy, sulfamoyl, hydroxyalkyl, amino groups; as well as its complexes with a bi- or trivalent metal ion having an atomic number from 20 to 31, 39, 42, 43, 44, 49, or from 57 to 83, as well as its salts with anions of physiologically acceptable organic acids chelated complexes of these compounds are used as contrast agents for nuclear magnetic resonance imaging.

Abstract: Wurster's crown ligands comprise a macrocyclic ligand such as a crown ether in which a hetero atom is substituted with a 1,4-phenylenediamine group. The phenylenediamine group is covalently bound to the macrocyclic ligand by one or both of the amine nitrogens, the amine nitrogen thereby substituting for the hetero atom of the macrocyclic ligand. The resulting compounds are redox active. Methods of making and using the compounds are also disclosed.