Abstract: Provided herein are optically active compounds of the formulae (ii); and (III) and pharmaceutical compositions thereof. Also provided herein are processes of making these compounds and resolving the racemic mixture or the enrichment of same with in one of its enantiomers to provide (R)- and (S)-1-(3-(3-N,N-dimethylaminocarbonyl)phenoxyl-4-nitrophenyl)-1-ethyl-N,N?-bis(ethylene)phosphoramidate, and methods of treating cancer comprising administering such compounds.

Abstract: A nucleoside analog and a salt thereof represented by any of the general formulae (1) to (10) below: wherein R1, R2, and R3 are the same or different groups, and each of the R1, R2 and R3 is selected from a hydrogen atom, a protecting group for a functional group in nucleic acid synthesis, a phosphate group, a phosphate group protected by a protecting group in nucleic acid synthesis, and an activated phosphate group for solid phase synthesis; and Ar is one of an aromatic hydrocarbon group and a polyaromatic hydrocarbon group.

Abstract: The oligophosphazene compound capable of forming a polymer which can be used as an optical material is a cyclic or linear compound including constituent units represented by the general formula (I) below in a range from 3 to 14. In the general formula (I), k is an integer of 1 to 4 and X1 is one selected from the group consisting of an oxygen atom, a sulfur atom, an NH group and an NCH3 group. A polymer made of this oligophosphazene compound exhibits high transparency and a high refractive index and is also less likely to cause optical dispersion, and thus it can be used as an optical lens, a retardation film, a light transmission body and other optical moldings.

Abstract: The inventions disclosed include methods of treating cancers and related neoplasias, especially prostate cancer, with pharmaceutically acceptable salts comprising lipophilic cation moieties linked to nitroxide or linked to hydroxylamine anti-oxidant groups.

Abstract: The present invention relates to a process for preparing stereoisomerically enriched 4-aryl-4-hydroxybutanoic acid derivatives by reducing 4-aryl-4-ketobutanoic acid derivatives in the presence of ruthenium-containing catalysts.

Abstract: There is disclosed an advantageous mixed acid anhydride production method of formula (1): R1C(O)OY(O)n(R2)p  (1) wherein R1, R2 and Y denote the same as defined below, n and p denote an integer of 1 or 2, which is characterized by adding a carboxylic acid of formula (2); R1COOH  (2) wherein R1 denotes a hydrogen atom, an optionally substituted alkyl group or the like, an organic base to a solution of a carboxylic acid activating agent of formula (3); (R2)pY(O)nX  (3) wherein R2 denotes an optionally substituted aliphatic hydrocarbyl group or the like, Y denotes a carbon atom, a phosphorus atom, or a sulfur atom, and X denotes a chlorine atom or the like.

Abstract: One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.

Abstract: This invention relates to a polymerizable phosphazene derivative with a general structural formula[.brket open-st.NP(A).sub.a (B).sub.b).brket close-st.]xwherein the groups A and B are bonded to phosphorus atoms through --O--, --S--, --NH--, or --NR-- (with R=C.sub.1 -C.sub.6) alkyl), and wherein A stands more precisely for a vinyl ether group or a styrene ether group, and B stands more precisely for a hydrocarbon group. The invention also relates to procedures for synthesizing such phosphazene derivatives. The phosphazenes derivatives of the invention can be cured by a process that is initiated cationically, which leads to a large number of advantages. The phosphazene derivatives of the invention can, in particular, be used as curable binders for paints, coatings, fillers, mastics, adhesives, moldings, or films. Paints or coatings comprising the phosphazene derivatives of the invention show especially high mechanical resistance and scratch resistance.

Abstract: This invention relates to a polymerizable phosphazene derivative with a general structural formula.brket open-st.NP(A).sub.a (B).sub.b).brket close-st..sub.xwherein the groups A and B are bonded to phosphorus atoms through --O--, --S--, --NH--, or --NR-- (with R=C.sub.1 -C.sub.6) alkyl), and wherein A stands more precisely for a vinyl ether group or a styrene ether group, and B stands more precisely for a hydrocarbon group. The invention also relates to procedures for synthesizing such phosphazene derivatives. The phosphazenes derivatives of the invention can be cured by a process that is initiated cationically, which leads to a large number of advantages. The phosphazene derivatives of the invention can, in particular, be used as curable binders for paints, coatings, fillers, mastics, adhesives, moldings, or films. Paints or coatings comprising the phosphazene derivatives of the invention show especially high mechanical resistance and scratch resistance.

Abstract: This invention relates to a polymerizable phosphazene derivative with a general structural formula.brket open-st.NP(A).sub.a (B).sub.b).brket close-st..sub.xwherein the groups A and B are bonded to phosphorus atoms through --O--, --S--, --NH--, or --NR-- (with R=C.sub.1 -C.sub.6) alkyl), and wherein A stands more precisely for a vinyl ether group or a styrene ether group, and B stands more precisely for a hydrocarbon group. The invention also relates to procedures for synthesizing such phosphazene derivatives. The phosphazenes derivatives of the invention can be cured by a process that is initiated cationically, which leads to a large number of advantages. The phosphazene derivatives of the invention can, in particular, be used as curable binders for paints, coatings, fillers, mastics, adhesives, moldings, or films. Paints or coatings comprising the phosphazene derivatives of the invention show especially high mechanical resistance and scratch resistance.

Abstract: Novel N-sulfinyl-2-carboxyaziridine compounds and novel N-hydrogen-2-hydroxymethylaziridine compounds are provided. The asymmetric synthesis of N-sulfinylaziridines is readily accomplished in high diastereomeric purity and good yield by the Darzens-type reaction of the metal enolate of an .alpha.-haloester and an enantiopure sulfinimine. Ring-opening of these aziridines affords .alpha.-amino acids and the otherwise difficult to prepare syn-.beta.-hydroxy-.alpha.-amino acids, both key structural units found in many bioactive materials. The N-sulfinyl radical may be selectively removed from the novel aziridine compounds by treatment with acid or base. Alternatively, the N-sulfinyl radical may be oxidized to provide the corresponding N-sulfonyl-aziridine, or reduced to form the corresponding 1H-2-hydroxymethylaziridine, either of which may subsequently be ring-opened to provide precursors to bioactive compounds.

Abstract: A process for the preparation of an oxirane, aziridine or cyclopropane of formula (I) wherein, X is oxygen, NR.sup.4 or CHR.sup.5 ; R.sup.1 is hydrogen, alkyl, aryl, heteroaromatic, heterocyclic or cycloalkyl; R.sup.2 is hydrogen, alkyl, aryl, heteroaromatic, CO.sub.2 R.sup.8, CHR.sup.14 NHR.sup.13, heterocyclic or cycloalkyl; or R.sup.1 and R.sup.2 join together to form a cycloalkyl ring; R.sup.3 is hydrogen, alkyl, aryl, heteroaromatic, CO.sub.2 R.sup.8, R.sup.8.sub.3 Sn, CONR.sup.8 R.sup.9 or trimethylsilyl; R.sup.4 and R.sup.5 are, independently, alkyl, cycloalkyl, aryl, heteroaromatic, SO.sub.2 R.sup.8, SO.sub.3 R.sup.8, COR.sup.8, CO.sub.2 R.sup.8, CONR.sup.8 R.sup.9 or CN, or R.sup.4 can also be P(O)(aryl).sub.2 ; R.sup.8 and R.sup.9 are independently alkyl, aryl or arylalkyl; R.sup.13 and R.sup.14 are independently hydrogen, alkyl or aryl; the process comprising reacting a mixture of a compound of formula (II), wherein R.sup.1, R.sup.2 and X are as defined above, and a sulphide of formula SR.sup.6 R.

Abstract: Compounds of the formula I ##STR1## in which R signifies a possibly substituted amino group of the general formula --NR.sup.1 R.sup.2, whereby, independently of one another, R.sup.1 and R.sup.2 each signify hydrogen, lower alkyl, lower alkenyl or lower alkynyl or R represents a saturated, unsaturated or aromatic heterocyclic ring which can possibly be substituted once or twice by lower alkyl or halogen, alk signifies a valency bond, a methylene, a saturated or unsaturated, straight-chained or branched alkylene chain with 2-6 carbon atoms and R.sup.3, R.sup.4 and R.sup.5, in each case independently of one another, signify hydrogen, lower alkyl or benzyl, as well as their pharmacologically acceptable salts and enantiomers, whereby, for the case that R.sup.3 =R.sup.4 =R.sup.5 =CH.sub.3 and alk signifies a valency bond, R cannot be the dimethylamino group, processes for their preparation and medicaments which contain these compounds for the treatment of calcium metabolism diseases.

Abstract: A stable lyophilized composition of the antitumor alkylating agent thiotepa and a method of preparing such a composition via co-lyophilization of the active ingredient with a pharmaceutical acceptable alkalizing agent.

Abstract: The present invention provides compounds having the structure: ##STR1## or having the structure: ##STR2## The present invention also provides a pharmaceutical compostion containing the compounds, methods of synthesizing the compounds, as well as methods of inhibiting growth of tumor cells and of treating a subject having a disease characterized by the proliferation of tumor cells.

Abstract: Compounds of the general formula: ##STR1## are useful as surfactants in the preparation of fluorocarbon emulsions, which can be used as oxygen-carrying blood substitutes, and for many other therapeutic and diagnostic applications. They are further useful in liposomal formulations which are themselves therapeutic agents or provide a vehicle for such agents.

Abstract: This disclosure describes an improved process for preparing N,N', N"-triethylenethiophosphoramide by the in situ generation of ethyleneimine.

Abstract: A method of inhibiting the replication of tumor cells is disclosed wherein Novel bis (2,2-dimethyl-1-aziridinyl)phosphinic amide antineoplastic agents of the formula: ##STR1## wherein X is R and R' are each, independently, hydrogen, alkyl, substituted alkyl, phenyl and substituted phenyl, Y is alkyl or substituted alkyl of 1-10 carbon atoms and, Z is oxygen or sulfur is administered to tumor cells.

Abstract: The binder/charge adhesive of the present invention makes it possible to improve the bonding between the charges and the polyurethane binder of a propellent composition. This agent is an aminoaziridinylphosphine oxide of general formula: ##STR1## in which R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are identical or different and denote a hydrogen atom or a methyl or ethyl radical. The present invention finds application particularly in the field of the manufacture of solid propellent compositions.

Abstract: Novel phosphoaziridines of the formula: ##STR1## wherein Z is oxygen or sulfur, R.sub.1 is independently at each occurrence H or --CH.sub.3, R.sub.2 is independently at each occurrence --CH.sub.3 or nitrophenyl R.sub.5 ; R.sub.3 is --NHR.sub.4, --OR.sub.4, --SR.sub.4 or ##STR2## where R.sub.4 is a radical containing up to 30 atoms including at least one amine, ester, ether, alkyl, substituted alkyl, hydrogen, phenyl, substituted phenyl, carbamate, heterocyclic ring or R.sub.5 group; provided that, when R.sub.4 contains and R.sub.5 group, R.sub.4 has an alkyl group between the phosphorous and the R.sub.5 group; and R.sub.5 is a radical containing and electron affinic group comprising a quinone, or a heterocyclic or phenyl ring directly connected to a radical selected from the group consisting of nitro, nitroso, sulfinyl, sulfoxine, and N-oxide; provided that the compound contains at least one R.sub.5 radical and provided that when R.sub.1 is H, the R.sub.2 group on the same ring is R.sub.