Patent classifications
C07F9/4006
PRODRUGS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA) INHIBITOR
Methods and compounds are disclosed for treating a disease or condition by inhibiting PSMA (Prostate Specific Membrane Antigen) using prodrugs of 2-PMPA
ISOQUINOLINONE COMPOUND FOR INHIBITING SSAO/VAP-1, AND USE THEREOF
An isoquinolinone compound acts as an inhibitor of semicarbazide-sensitive oxidase (SSAO) and/or vascular adhesion protein-1 (VAP-1), and the use thereof, and further relates to a pharmaceutical composition containing the compound. The compound or the pharmaceutical composition can be used to prepare a drug for preventing, treating or ameliorating inflammation and/or inflammation-related diseases, diabetes and/or diabetes-related diseases in patients, and especially can be used to prepare a drug for preventing, treating or ameliorating non-alcoholic fatty liver diseases in patients.
Amino- or ammonium-containing sulfonic acid, phosphonic acid and carboxylic acid derivatives and their medical use
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##
Stable ligand mixtures and processes for making same
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 and methods for treating cancer
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.
Organophosphorus compounds for flame retardant polyurethane foams
An organophosphorus compound useful in a phosphorus containing flame retardant and a flame retardant polyurethane foam, where the organophosphorus compound is shown in Formula (I) where Y is selected from the group consisting of an —OH group, an —NH.sub.2 group, an —NHR.sup.3 group, and an —SH group, where R.sup.3 is a monovalent hydrocarbyl group having 1 to 10 carbon atoms; R is a divalent hydrocarbyl group; X is a heteroatom group; and R.sup.1 and R.sup.2 are each independently a substituted or unsubstituted hydrocarbyl group, wherein R.sup.1 and R.sup.2 can be optionally joined to form a ring. ##STR00001##
PRODRUGS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA) INHIBITOR
Methods and compounds are disclosed for treating a disease or condition by inhibiting PSMA (Prostate Specific Membrane Antigen) using prodrugs of 2-PMPA.
USE OF AMINO-CONTAINING NEUTRAL PHOSPHINE EXTRACTANT IN EXTRACTION AND SEPARATION OF THORIUM AND PROCESS OF USING SAME
The present invention relates to use of an amino-containing neutral phosphine extractant of Formula I in extraction and separation of thorium, and a process of extracting and separating thorium using the amino-containing neutral phosphine extractant of Formula I,
##STR00001##
wherein, R.sub.1 and R.sub.2 are each independently selected from the group consisting of C.sub.1-C.sub.12 alkyl, R.sub.3 and R.sub.4 are each independently selected from the group consisting of C.sub.1-16 alkyl and hydrogen, and n is an integer of 1 to 8.
THYROID HORMONE RECEPTOR AGONIST AND USE THEREOF
A thyroid hormone receptor agonist and its use in the treatment of a disease associated thyroid hormone receptor beta are described. The compound can be effective in lowering cholesterol with minimum or no adverse effects on the heart or thyroid hormone axis.
Process for preparing sulfonamide compounds
The present invention relates to a process for preparing a sulfonamide compound which is an inhibitor of Bcl-2/Bcl-xL, including the compound (3R)-1-(3-(4-(4-(4-(3-(2-(4-chlorophenyl)-1-isopropyl-4-methylsulfonyl-5-methyl-1H-pyrrol-3-yl)-5-fluorophenyl)piperazine-1-yl)-phenylaminosulfonyl)-2-trifluoromethanesulfonyl-anilino)-4-phenylthio-butyl)-piperidine-4-carboxylic acid 3-phosphonopropyl ester. The present invention also relates to an intermediate for preparing the sulfonamide compound and a preparation process thereof.