Abstract:
The novel bisphosphonic acid ester derivatives represented by the following formula (1): Y—Cy—(NH)m—(CH2)n—C(X)(PO(OR1)(OR2))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.
Abstract:
The invention relates to the process for preparing ethylenedialkylphosphinic acids, esters and salts, wherein a) a phosphonic acid source (I) is reacted with olefins (IV) in the presence of a catalyst A to give an alkylphosphonous acid (II), or salt or ester thereof, b) the alkylphosphonous acid (II), or the salt or ester thereof, is reacted with an acetylenic compound (V) in the presence of a catalyst B to give the ethylenedialkylphosphinic acid derivative (III) where R1, R2, R3, R4, R5, R6, R11, R12, R13, R14 are the same or different and are each independently H, C1-C18-alkyl, C6-C18-aryl, C6-C18-aralkyl, C6-C18-alkylaryl, where the C6-C18-aryl, C6-C18-aralkyl, C6-C18-alkylaryl groups may be substituted by —C(O)CH3, OH, CH2OH, NH2, NO2, OCH3, SH and/or OC(O)CH3, and X is Mg, Ca, Al, Sb, Sn, Ge, Ti, Fe, Zr, Zn, Ce, Bi, Sr, Mn, Cu, Ni, Li, Na, K, H and/or a protonated nitrogen base, and/or is H, C1-C18-alkyl, C6-C18-aryl, C6-C18-aralkyl, C6-C18-alkylaryl, (CH2)kOH, CH2—CHOH—CH2OH, (CH2)kO(CH2)lH, (CH2)k—CH(OH)—(CH2)lH, (CH2—CH2O)kH, (CH2—C[CH3]HO)kH, (CH2—C[CH3]HO)k(CH2—CH2O)lH, (CH2—CH2O)k(CH2—C[CH3]HO)H, (CH2—CH2O)k-alkyl, (CH2—C[CH3]HO)k-alkyl, (CH2—C[CH3]HO)k(CH2—CH2O)l-alkyl, (CH2—CH2O)k(CH2—C[CH3]HO)O-alkyl, (CH2)kNH2, (CH2)kN[(CH2)lH]2, where k and l are the same or different and are each independently an integer from 0 to 20, and m is 1 to 4, and the catalyst A comprises transition metals and/or transition metal compounds and/or catalyst systems composed of a transition metal and/or a transition metal compound and at least one ligand, and the catalyst B comprises electromagnetic radiation.
Abstract:
A non-aqueous electrolyte composition containing (i) at least one aprotic organic solvent; (ii) a compound of formula (I) (iii) at least one ion containing conducting salt; and (iv) optionally one or more additives.
Abstract:
This invention relates to compounds that inhibit creatine transport and/or creatine kinase, pharmaceutical compositions including such compounds, and methods of utilizing such compounds and compositions for the treatment of cancer.
Abstract:
This invention pertains to the use of fused bicycle heterocyclic adducts of thiohydroxy pyridines or pyrimidines as diacylglycerol O-acyltransferase 1 (DGAT-1) inhibitors to treat hyperlipidiemias and various diseases and disorders associated therewith. Other conditions also be ameliorated or avoided, such as high postprandial triglycerides or diet-related hypertriglyceridemia, cardiovascular risk associated with excessive triglycerides, and insulin resistance/glucose intolerance in overweight patients, those with diabetes or other glucose metabolic disorders such as Syndrome X and/or polycystic ovary disease.
Abstract:
β-Substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.
Abstract:
Mixtures of diphosphinic acids and alkylphosphinic acids, a process for preparation thereof and use thereofThe invention relates to mixtures of at least one diphosphinic acid of the formula (I) in which R1, R2 are each H, C1-C18-alkyl, C2-C18-alkenyl, C6-C18-aryl, C7-C18-alkylaryl R4 is C1-C18-alkylene, C2-C18-alkenylene, C6-C18-arylene, C7-C18-alkylarylene with at least one alkylphosphinic acid of the formula (II) in which R3 is C1-C18-alkyl, C2-C18-alkenyl, C6-C8-aryl, C7-C18-alkylaryl. The invention also relates to a process for preparing these mixtures and to the use thereof.
Abstract:
The invention relates to a method for producing ethylenedialkylphosphinic acids, esters and salts, and to the use thereof as flame retardants. The claimed method is characterised in that •a) a phosphinic acid source (I) is reacted with olefins (IV) in the presence of catalyst A so as to obtain an alkylphosphonous acid, salt or ester (II) thereof, and •b) the alkylphosphonous acid, salt or ester (II) thereof obtained in this manner is reacted with acetylenic compound (V) in the presence of catalyst B in order to obtain the ethylenedialkylphosphinic acid derivative (III), •catalyst A being transition metals and/or transition metal compounds and/or catalyst systems composed of a transition metal and/or a transition metal compound and at least one ligand •and catalyst B being electromagnetic radiation.
Abstract:
The invention pertains to the use of fused bicyclo heterocyclic adducts of thiohydroxy pyridines or pyrimidines as diacylglycerol O-acyltransferase 1 (DGAT-1) inhibitors to treat hyperlipidiemias and various diseases and disorders associated therewith. Other conditions also can be ameliorated or avoided, such as high postprandial triglycerides or diet-related hypertriglyceridemia, cardiovascular risk associated with excessive triglycerides, and insulin resistance/glucose intolerance in overweight patients, those with diabetes or other glucose metabolic disorders such as Syndrome X and/or polycystic ovary disease.
Abstract:
Compounds and compositions are provided that inhibit histone deacylase activity and which expand renal progenitor cell populations and improve kidney function in a damaged kidney. Methods of use of the compounds and compositions are provided.