Phosphonate linkers and their use for delivering compounds with passive cell permeability into a cell wherein the phosphonate group facilitates cellular retention of the compound are described.

Phosphonate linkers and their use for delivering compounds with passive cell permeability into a cell wherein the phosphonate group facilitates cellular retention of the compound are described.

The present invention relates to amino- or ammonium-containing sulfonic acid, phosphonic acid and carboxylic acid derivatives, in particular the compounds of formula 1, 2, 3, 4, 5 or 6, and their medical use, including their use in the treatment, prevention or amelioration of an inflammatory, autoimmune and/or allergic disorder. ##STR00001##

The novel bisphosphonic acid ester derivatives represented by the following formula (1):

Y—Cy—(NH).sub.m—(CH.sub.2).sub.n—C(X)(PO(OR.sup.1)(OR.sup.2)).sub.2   (1)

wherein each symbol is as defined in the DESCRIPTION, which has an amino group substituted by a heterocyclic group or a heterocyclic group containing a nitrogen atom, and the acid moiety is esterified with a POM group, an n-butanoyloxymethyl (BuOM) group and the like, exhibit a superior direct or indirect cytotoxicity effect on tumor cells and virus infected cells.

A process of stabilizing a bidentate or tridentate phosphorus-based phosphite ester ligand or mixture thereof in a hydrocyanation reaction milieu comprising water, wherein the ligand or ligand mixture comprises one or more of (i) a bidentate biphosphite ligand of formula (III), (R.sup.12—X.sup.12) (R.sup.13—X.sup.13) P—X.sup.14—Y—X.sup.24—P(X.sup.22—R.sup.22) (X.sup.23—R.sup.23) or (ii) a tridentate triphosphite ligand of formula (IIIA) (R.sup.12—X.sup.12) (R.sup.13—X.sup.13) P—X.sup.14—Y—X.sup.32—P(X.sup.34—R.sup.34)—(X.sup.33—Y.sup.2—R.sup.24—P(X.sup.23—R.sup.23)—(X.sup.22—R.sup.22) where each X is oxygen or a bond and each Y is an optionally substituted C6-C20 arylene group, comprising admixing the bidentate and/or tridentate with a stabilizing amount of one or more monodentate phosphite ligand of formula P(X.sup.1—R.sup.1)(X.sup.2—R.sup.2)(X.sup.3—R.sup.3) where each X is oxygen or a bond, wherein the monodentate ligand has a rate of hydrolysis greater than the rate of hydrolysis of the bidentate or tridentate ligand in the presence of water in a hydrocyanation reaction milieu, and thereby preserve concentrations and proportions of the bidentate and/or tridentate ligand(s) in the ligand blend.

Silylalkyloxyaryl compounds useful as anti-cancer agents. The compounds and pharmaceutical compositions containing them are particularly useful for the treatment of melanoma, colon, neuroblastoma, bladder, breast, lung, pancreatic, melanoma, sarcoma, lymphoma or gastric cancer.

The disclosure provides a compound comprising bisphosphonate functional group and chelating agent. The bisphosphonate functional group part has high affinity for bone tissue, and the chelating agent part has high affinity for metal tracer such as radioisotope. The disclosed compound could be rapidly adsorbed onto the bone surface, and could steady emit ionizing radiation. Therefore, the disclosed compound is suitable for bone scanning technology to find abnormalities in bone.

The subject matter disclosed herein relates to compositions and methods of making and using the compositions. In a further aspect, the subject matter disclosed herein relates to inhibitors of STAT3 dimerization. Methods of making these compositions as well as compositions comprising these compositions are also disclosed. Also disclosed are methods of treating or preventing certain cancers by administering to an individual in need thereof and effective amount of the compounds disclosed herein. Still further, disclosed herein are methods of inhibiting STAT3 by contacting a cell with a compound or composition as disclosed herein.

Provided are a near-infrared-ray-absorbing composition having strong near-infrared shielding properties when a cured film is produced, a near-infrared-ray cut filter, a manufacturing method therefor, a camera module, and a manufacturing method therefor. The near-infrared-ray-absorbing composition includes a copper complex obtained by reacting a compound (A) having at least two coordination sites with a copper component.

The invention provides synthetic processes and synthetic intermediates that can be used to prepare compounds having useful anti-HIV properties.