Abstract: Conjugates of transferrin, albumin and polyethylence glycol consisting of native or thiolated transferrin or albumin or of polyethylene glycol (MW between approximately 5,000 and 20,0000) with at least one HS—, HO— or H2N group and cytostatic compounds derived through maleinimide or N-hydroxysuccinimide ester compounds, such as doxorubicin, daunorubicin, epirubicin, idarubicin, mitoxandrone, chloroambucil, melphalan, 5-fluorouracyl, 5′-desoxy-5-fluorouridine, thioguanine, methotrexate, paclitaxel, docetaxel, topotecan, 9-aminocamptothecin, etoposide, teniposide, mitopodoside, vinblastine, vincristine, vindesine, vinorelbine or a compound of general formula A, B, C or D, where n=0-6, X=—NH2, —OH, —COOH, —O—CO—R—COR*, —NH—CO—R—COR*, where R is an aliphatic carbon chain with 1-6 carbon atoms or a substituted or unsubstituted phenylene group and R* H, phenyl, alkyl with 1-6 carbon atoms.

Abstract: A novel pharmaceutical composition, comprising cisplatin and folic acid is disclosed. The preparation of this pharmaceutical composition is also disclosed. The composition may be used to treat cancers and Acquired Immune Deficiency Syndrome (AIDS).

Abstract: Novel folic acid derivatives and their use in preparation of &ggr;-esters of folic acid via a pteroyl azide intermediate are described. Folic acid &ggr;-esters are useful intermediates in the synthesis of folic acid conjugates capable of binding folate receptors in vitro and in vivo.

Abstract: The present invention relates to an organic controller capable of controlling redox reaction at a low cost in a simple manner, the organic controller comprising a combination of two or more substances selected from vitamins and vitamin-like substances, a combination of one or more substances selected from vitamins and vitamin-like substances and one or more substances selected from polyphenols, a combination of one or more substances selected from vitamins and vitamin-like substances and one or more substances selected from enzymes, or a combination of one or more substances selected from vitamins and vitamin-like substances, one or more substances selected from polyphenols and one or more substances selected from enzymes, as the effective component.

Abstract: A nutritional supplement for improving cardiovascular health via aiding in preventing, delaying the onset of and/or slowing the progression of atherosclerosis and coronary heart disease, the supplement comprising one or more flavonoids and folic acid or folate; and a method for aiding in preventing, delaying the onset of and/or slowing the progression of atherosclerosis and coronary heart disease are described.

Abstract: Corticotropin releasing factor (CRF) antagonists of formula (I): ##STR1## and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.

Abstract: A composition for human or animal consumption for supplying folate which includes a natural isomer of reduced folate, such as (6S)-tetrahydrofolic acid, 5-methyl-(6S)-tetrahydrofolic acid, 5-formyl-(6S)-tetrahydrofolic acid, 10-formyl-(6R)-tetrahydrofolic acid, 5,10-methylene-(6R)-tetrahydrofolic acid, 5,10-methenyl-(6R)-tetrahydrofolic acid, 5-formimino-(6S)-tetrahydrofolic acid, and their polyglutamyl derivatives is disclosed. Such compositions include multivitamin preparations (with or without minerals and other nutrients); breakfast foods such as prepared cereals, toaster pastries and breakfast bars; infant formulas; dietary supplements and complete diet and weight-loss formulas and bars; animal feed (for example pet foods) and animal feed supplements (such as for poultry feed). The amount of the natural isomer of a reduced folate in a composition for human consumption can range between about 5% and about 200% of the daily requirement for folic acid per serving or dose.

Abstract: The present invention relates to the use of pteridine derivatives of the formula I ##STR1## in which X is O, NH or N--(C.sub.1-C.sub.5)-alkanoyl, R.sup.3 is the radical --OR.sup.4, --NR.sup.5 R.sup.6 or --S(O).sub.m R.sup.7, and R, R.sup.1, R.sup.2, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and m have the meanings given in claim 1, which are nitric oxide synthase inhibitors, for the treatment of diseases which are caused by an increased nitric oxide level.

Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.

Abstract: Inhibitor of the use of tetrahydrobiopterin as a cofactor for nitric oxide synthase, e.g., substituted 4-phenyl(hydropyridines) such as 1-methyl-4-(3',4'-dihydroxyphenyl)-1,2,3,6-tetrahydropyridine or, 4-(3',4'-dihydroxyphenyl)-1,2,3,6-tetrahydropyridine) or tetrahydropterin analog which does not replace tetrahydrobiopterin as a substrate for nitric oxide synthase such as (6R,S)-6,7-dimethyl-tetrahydropterin or (6R,S)-tetrahydrofolic acid or 2,4-diamino-, 2,6-diamino, or 4,6-diamino mono- or disubstituted pyrimidines or the corresponding pyrimidine-3-oxides such as 2,4-diamino-6-(diethylamino)pyrimidine, 2,4-diamino-6-piperidino-pyrimidine-3-oxide, 2,4-diamino-6-hydroxypyrimidine, 4,6-diamino-2-hydroxypyrimidine or 2,5-diamino-4,6-dihydroxypyrimidine is administered to inhibit nitric oxide synthesis from arginine in vascular cells in a subject in need of such inhibition (e.g., for prophylaxis or treatment of cytokine- or endotoxin-induced hypotension (e.g., septic shock).

Abstract: Compounds of general formula I and their salts and solvates are antifungal agents and as such are useful in the treatment of various fungal infections. Pharmaceutical compositions including these compounds and processes for their preparation are also provided.

Abstract: This invention is directed to bicyclic pyrimidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.

Abstract: The present invention refers to the use of 5-methyltetrahydrofolic acid, of 5-formyltetrahydrofolic acid and of their pharmaceutically acceptable salts for the preparation of controlled release pharmaceutical compositions suitable for the use in the therapy of depressive disturbances, in particular major depression, dysthymia or depressive neurosis and not otherwise specified depressive disturbances, independently from folate plasmatic levels, and to the pharmaceutical composition thus prepared.

Abstract: A phenylalanine-glycine derivative of the general formula (I): ##STR1## wherein R represents a residue of an antitumor substance, or a salt or ester thereof, a process for preparation thereof, and a pharmaceutical composition containing the same are described.The novel conjugate of the phenylalanine-glycine derivative and the antitumor substance exhibits superior antitumor activity in comparison with the case wherein an antitumor substance is administered singly or as a mixture with phenylalanine.

Abstract: The present invention is directed to a novel process for the production of folic acid in high yield utilizing a novel diimine as an intermediate. This diimine is formed by reacting 2-substituted malondialdehyde with p-aminobenzoyl-L-glutamic acid. This diimine may be converted into folic acid by reacting said diimine with triaminopyrimidinone in the presence of sulphite.

Abstract: A novel prolinal derivative of the general formula: ##STR1## [wherein A represents alkylene or alkenylene group of from 1 to 8 carbon atom(s) or a saturated hydrocarbon ring of from 3 to 7 carbon atoms, R represents hydrogen atom, phenyl group, benzyl group, alkyl group of from 1 to 8 carbon atom(s) or cycloalkyl group of from 3 to 7 carbon atoms,B represents alkylene group of from 1 to 8 atom(s) unsubstituted or substituted by phenyl group or benzyl group, or a single bond,D represents carbocyclic or heterocyclic ring unsubstituted or substituted by from one to three of halogen atom, alkyl or alkoxy group of from 1 to 4 carbon atom(s), nitro group or trifluoromethyl group.]possess inhibitory activity on prolyl endopeptidase, and therefore are useful for treating and/or preventing agent as a amnesia.

Abstract: This invention is directed to novel nucleophilic polysubstituted aryl acridinium esters and to novel conjugates thereof. The novel nucleophilic polysubstituted aryl acridinium esters and novel conjugates thereof are useful in biological assays, including novel assays for the determination of Vitamin B.sub.12, folate, cortisol, estradiol, and thromboxane B.sub.2.

Abstract: Intermediates and a process for the synthesis of 6-monosubstituted tetrahydropteridine C6-stereoisomers, including (6S)-tetrahydrofolic acid. The intermediates are shown in their two enantiomeric forms as follows: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and represent hydrogen, methyl, hydroxy, amino, alkyl or dialkylamino, alkoxy, benzyloxy, or benzylthio; R.sub.3 represents an alkene, alkyne, cycloalkyl, benzyl, alkyl (substituted with hydroxy, acetoxy, benzyloxy, alkoxy, alkylthio, amino, carboxy, oxo, or phosphate), a protected aldehyde, or ##STR2## wherein n=1 or 2, R.sub.4 is hydrogen, formyl, methyl, or propargyl, and ZZ represents an amino acid or amino acid polymer. Also, a process for tetrahydropteridine N5-formylation for the preparation of, for example, N5-formyl-(6S)-tetrahydrofolic acid.

Abstract: 6,6-Disubstituted pteridines which are useful for the regulation of enzymes are disclosed, along with a general method of synthesizing these compounds.

Abstract: An anthraquinone type compound which is represented by the following general formula (I) and which exhibits yellow to orange-colored hue; and a composition for liquid crystal display element obtained by dissolving the compound into liquid crystal: ##STR1## (where: X.sup.1 and X.sup.2 denote sulfur or selenium; and R.sup.1 and R.sup.2 represent a substituted or unsubstituted phenyl group, a substituted or unsubstituted naphthyl group, a substituted or unsubstituted pyridyl group, a substituted or unsubstituted pyrmidyl group or a tetrahydronaphthyl group, with the following exceptions:(1) X.sup.1 =X.sup.2 =S; R.sup.1 =R.sup.2 =a substituted or unsubstituted phenyl group =(2) X.sup.1 =X.sup.2 =S; R.sup.1 =a substituted or unsubstituted naphthyl group; R.sup.2 =a phenyl group or a naphthyl group(3) X.sup.1 =X.sup.2 =Se; R.sup.1 =R.sup.2 =a tetrahydronaphthyl group).

Abstract: This invention relates to a stabilized aqueous folic acid preparation which comprises a folic acid component selected from the group consisting of folic acid, ammonium, alkali metal and alkaline earth metal salts of folic acid and mixtures thereof, and which has an improved stability of its folic acid contents in the presence of oxygen, the said preparation containing as a stabilizer a combination of(a) at least one member selected from the group consisting of dihydrofolic acid and ammonium, alkali metal, alkaline earth metal and alkanolammonium salts thereof, and(b) at least one member selected from the group consisting of at least one hydroxypolycarboxylic acid and ammonium, alkali metal, alkaline earth metal and alkanolammonium salts thereof.

Abstract: 2,4-Diaminopteridine derivatives and the pharmaceutically acceptable salts thereof having potent anticancer activity are disclosed. The derivatives possess the structural formula: ##STR1## wherein Y is NH.sub.2, OH or SH, R is ##STR2## and X is ##STR3## in which R' is H or CH.sub.3 or ##STR4## in which R and R' are as previously defined, provided when Y is NH.sub.2, R' must be CH.sub.3 and when Y is OH, R' must be OH.

Abstract: Novel purine derivatives, particularly novel guanines and hypoxanthines, are described as agents for treating autoimmune diseases. Also novel methods of manufacture for the derivatives, pharmaceutical compositions thereof, and methods of use therefor are the invention.

Abstract: A sensitive intermediate metabolite such as a folic acid derivative or analog is stabilized by complexing it with a complementary binder or receptor such as a protein and then lyophilizing the complex. An example of such a folic acid derivative is N-5-methyltetrahydrofolic acid.

Abstract: Novel protein conjugates and radioiodinated derivatives of folic acid and salts, esters and amides useful in the radioimmunoassay (RIA) of body fluids to determine folic acid are disclosed.

Abstract: Novel selenium-75 derivatives of folates, which are useful in competitive radio assay of folates, have the general formula: ##STR1## where a dotted bond line indicates that the bond may be single or double, and whereX is H or --CH.sub.3,m is 0 or 1 (such that the adjacent nitrogen atom is trivalent), and either(a) R is ##STR2## and is attached through the nitrogen atom to the pteroyl residue where q is 0 or 1p is 1 or 2Q is C.sub.x H.sub.2x+1 where x is from 1 to 6and when q is 0, Z is H and when q is 1, Z is HO, or(b) R is--CO.CHY.CHY.CH(COOH)NH--and is attached through the nitrogen atom to the pteroyl residue, where Z is HO,one group Y is --H and the other group Y is --SeC.sub.x H.sub.2x+1 where x is from 1 to 6 and esters and salts of such acid.