Patent classifications
C07F15/0053
MANUFACTURE OF TRANS-[TETRACHLOROBIS(1H-INDAZOLE)RUTHENATE (III)] AND COMPOSITIONS THEREOF
The present invention relates to the preparation of compositions comprising sodium trans-[tetrachlorobis(1H-indazole)ruthenate (III)]. Synthesis and formulation preparation is detailed. Impurity profiles are also discussed. Compositions herein are useful for anti-cancer applications.
RUTHENIUM COMPLEX CONTAINING ALKYNYL GROUP, METHOD OF SYNTHESIZING THE SAME AND USE THEREOF
A Ruthenium complex containing alkynyl group, a method of synthesizing the Ruthenium complex containing alkynyl group and a use thereof are provided. The Ruthenium complex has a chemical formula of Ru(L).sub.2(DPPZ′). DPPZ′ is a main ligand having structural formula of
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R is any one selected from the group consisting of H, substituted or unsubstituted phenyl, R.sub.1NH.sub.2, R.sub.1OH, and SiMe.sub.3; R.sub.1 is C1-C5 chain alkyl group; L is an auxiliary ligand with N as coordinating atom. Sonogashira coupling reaction is utilized to introduce alkynyl group into a DPPZ-type Ruthenium complex; the introduced alkynyl group is beneficial to promote the transmembrane absorption of drug molecules, increase the probability of drug entry into cells, and can also increase efficacy and reduce toxic and side effects of drugs. The Ruthenium complex provided has significant anti-tumor activity, especially anti-breast cancer activity, and can provide new ideas for designing anti-tumor drug molecules in the future.
Chiral tetradentate ligand, method for producing same and transition metal complex of said chiral tetradentate ligand
The present invention relates to a compound represented by the formula (1.sup.A). G represents a group selected from the group consisting of a monovalent group represented by the formula (G.sup.P) and a monovalent group represented by the formula (G.sup.S). R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, and R.sup.12 each independently represent a hydrogen atom or a group selected from the group consisting of an alkyl group, an alkenyl group, an aryl group, an aralkyl group, an alkoxy group, a halogeno group, and a halogeno alkyl group. ##STR00001##
POTENT AND SELECTIVE INHIBITORS OF CYTOCHROME P450
Inhibitors of the enzyme cytochrome P450 (CYP), including 1B1 (CYP1B1), 1A1 (CYP1A1) and 19A1 (CYP19A1) are provided, and are useful in medical applications. Disclosed are highly potent and selective compounds that can be used in chemoprevention to ameliorate malignant changes induced by CYP, or to aid in treatment, including restoration of chemotherapeutic efficacy.
Catalytically highly effective precious metal-carboxylate compounds of Ir, Ru, Rh, Pd and Au
Processes produce catalytically highly effective noble metal carboxylate compounds or their solutions that comprise A) a noble metal carboxylate, wherein the noble metal is selected from the group consisting of ruthenium, platinum, palladium, rhodium and gold, and B) at least one compound selected from the group consisting of oxalic acid, a salt of oxalic acid, a derivative of oxalic acid and a salt of the derivative of oxalic acid. The process digests the noble metal with alkaline earth peroxide to produce a digestion mass and dissolves the digestion mass in a carboxylic acid or a carboxylic acid diluted with a protic solvent to produce a resulting solution, whereby alkaline earth ions are separated off as salt of an oxalic acid or salt of oxalic acid derivatives, and the processes do not include any BaSO4 precipitation and filtration of barium sulphate.
Ruthenium-based photolinkers and methods of use
The present invention provides ruthenium-based photolinker compounds, caged molecules comprising the ruthenium-based photolinker compounds, and methods of use. In certain aspects, the compositions disclosed herein comprise an active domain conjugated to a ruthenium-based photolinker, such that irradiation of the photolinker exposes the active domain.
Manufacture of trans-[tetrachlorobis(1H-indazole)ruthenate (III)] and compositions thereof
The present invention relates to the preparation of compositions comprising sodium trans-[tetrachlorobis(1H-indazole)ruthenate (III)]. Synthesis and formulation preparation is detailed. Impurity profiles are also discussed. Compositions herein are useful for anti-cancer applications.
PLATINUM COMPOUNDS FOR BINDING GUANINE QUADRUPLEXES
Compounds are described and characterized that bind guanine quadruplexes of DNA or RNA. Binding data and inhibition of growth data of five cancer cell lines are presented.
Transcriptome in vivo analysis (TIVA) and transcriptome in situ analysis (TISA)
Compositions and methods of capturing one or more nucleic acid molecules of a cell or subcellular compartment are described. In certain aspects, the compositions comprise a caged molecule comprising one or more photolinkers and an antisense oligonucleotide, which when uncaged hybridizes to a target nucleic acid molecule.
COMPOUND OF 3,3,3',3'-TETRAMETHYL-1,1'-SPIROBIINDANE-BASED PHOSPHINE LIGAND, AND PREPARATION METHOD THEREOF
The present application discloses a 3,3,3′,3′-tetramethyl-1,1′-spirobiindane-based phosphine ligand, an intermediate, a preparation method and uses thereof. The compound of phosphine ligand is a compound having a structure represented by formula I or formula II, or an enantiomer, a raceme, or diastereomer thereof. The phosphine ligand can be prepared via a preparation scheme in which the cheap and easily available 6,6′-dihydroxyl-3,3,3′,3′-tetramethyl-1,1′-spirobiindane is used as a raw material and the compound represented by formula III serves as the key intermediate. The new phosphine ligand developed by the present application can be used in catalytic organic reaction, in particular as a chiral phosphine ligand that is widely used in many asymmetric catalytic reactions including asymmetric hydrogenation and asymmetric allyl alkylation, and thus it has economic practicability and industrial application prospect.
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