Abstract: The synthesis of taxol and other tricyclic and tetracyclic taxanes.

Abstract: The reaction mixture obtained in the production of 2,3-epoxypropyltrialkylammonium chlorides by treatment of chlorohydroxypropyltrialkylammonium chlorides with alkaline acting materials in aqueous medium containing impurities which create problems in the subsequent use of the 2,3-epoxypropyltrialkylammonium chloride. According to the invention the reaction mixture is freed from these impurities by separating it from undissolved impurities by employing at least about 0.2 mole of 2,3-epoxypropyltrialkylammonium chloride per mole of water.

Abstract: The present invention relates to therapeutically active azaheterocyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a central nervous system ailment related to the GABA uptake.

Abstract: This is described an improved process for the asymetric synthesis of (+)-Pancratistatin utilizing aziridines as the starting materials.

Abstract: A compound of formula V: ##STR1## wherein all the R's groups are as defined in the specification, is useful in the treatment of bacterial infections.

Abstract: 2'- and/or 7'- substituted taxoid derivatives having improved water-solubility and/or enhanced therapeutic activity and methods of making the same are disclosed.

Abstract: This invention relates to a method of preparing taxane derivatives of formula (I) by esterification of protected baccatin III or 10-deacetylbaccatin III by means of an acid of formula (VII), elimination of protection groupings and acylation of the amine function of the side chain. The products of formula (I) have remarkable antitumor and antileukemia properties. In formulae (I) and (VII): Ar stands for aryl, R is hydrogen or acetyl, R.sub.1 is a benzoyl radical or an R.sub.2 --O--CO-- radical in which R.sub.2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl, R.sub.3 is a trihalomethyl radical or phenyl substituted by a trihalomethyl radical, R.sub.4 is a hydrogen atom or is the same as R.sub.1.

Abstract: Process for the synthesis of taxol and other tricyclic and tetracyclic taxanes.

Abstract: A method of preparing cyclic formals which contain only small amounts of by-product impurities and unreacted starting materials, and which are ready to be purified.In preparing a cyclic formal by reacting alkylene glycol with formaldehyde in the presence of a catalyst, a reaction vessel provided with a vapor-liquid contact zone at the upper part thereof is used. Vapor generated from the reaction mixture and containing a cyclic formal goes up and passes through the vapor-liquid contact zone to be condensed. While part of the condensate is returned to the vapor-liquid contact zone, the remainder of the condensate is taken out as a distillate.

Abstract: The present invention concerns photochemical labelling reagents comprising a digoxigenin derivative and a furocoumarin derivative bound via a spacer. The labelling reagent can be used in gene diagnostic.

Abstract: The present invention is a method of preventing or reducing atherosclerosis or restenosis, and a pharmaceutical preparation used therefor. In particular, it is a method of preventing or reducing atherosclerosis or restenosis after arterial injury by treatment with a low dose of a microtubule stabilizing agent such as taxol or a water soluble taxol derivative. The low dose used in the present invention prevents artery blockage while minimizing any negative side effects associated with the drug.

Abstract: This invention relates to a method of preparing taxane derivatives of general formula (I) by esterification of protected baccatine III or 10-deacetylbaccatine III by means of an acid of general formula (VII), elimination of protection groupings of the ester obtained, and acylation of the amine function of the side chain. In formulae (I) and (VII): Ar stands for aryl, R is hydrogen or acetyl, R.sub.1 is benzoyl or R.sub.2 --CO--O-- in which R.sub.2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl, R.sub.3 and R.sub.4 may be the same or different and represent hydrogen, alkyl, alkenyl, aralkyl, aryl or alkoxy, and R.sub.5 is an alkyl radical substituted by one or more chlorine atoms (2,2,2-trichloroethyl, (2-trichloromethylisopropyl).

Abstract: Water-soluble prodrugs of the formula: ##STR1## wherein: D is a biologically active nucleophile;M is X or Q;x is an electron withdrawing group;Q is a moiety containing a free electron pair positioned five or six atoms from Y';Y and Y' are oxygen or sulfur;R is a polyalkylene oxide; andZ is OH, C.sub.1-4 alkyl moieties or ##STR2## are disclosed.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydroxy, 2-hydroxyethoxy, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkanoyloxy, halogen, amino, azido, a keto, p-nitrobenzenesulfonyl or a pyranyloxy group of the formula ##STR2## wherein X is a group of the formula ##STR3## wherein R.sub.3 is hydroxy, C.sub.1 -C.sub.4 alkanoyloxy or organic sulfonyloxy, andR.sub.4 is hydroxy or carbamoyloxy,R.sub.2 is hydrogen, hydroperoxy, hydroxy or methoxy,Y is a group of the formula ##STR4## wherein R.sub.5 is hydroxy or C.sub.1 -C.sub.4 alkanoyloxy, andR.sub.6 and R.sub.7 each independently of the other is hydrogen or methyl, are suitable for the preparation of a medicament for the prophylaxis and treatment of diseases that respond to the inhibition of the osteoclast proton pump.

Abstract: Alkaline sensitive protaxol is water soluble and is hydrolyzed at physiological (alkaline) pH to render the native taxol structure and the native taxol activity. Protaxol compositions include 2'- and/or 7-O-ester derivatives of taxol and/or 2'- and/or 7-O-carbonate derivatives taxol. Protaxol has a formula as follows: ##STR1## wherein R.sup.1 and R.sup.2 are each H or a radical selected from the group consisting of --CO--(CH.sub.2).sub.m --X--(CH.sub.2).sub.n --COZ and --COO--(CH.sub.2).sub.o --Y--Ar, and wherein m, n, and o are each an integer of 1 to 3; X is O, S, NH, SO, or SO.sub.2 ; Y is S, SO or SO.sub.2 ; Ar is phenyl or substituted phenyl wherein the substituent is halo, amino, nitro or N,N-dialkylamino having 1 to 4 carbons in each of the alkyl groups; and Z is OH, OR.sup.3, SR.sup.3 or NR.sup.4 R.sup.5 wherein R.sup.3 is alkyl containing 1 to 4 carbons and R.sup.4 and R.sup.

Abstract: This invention relates to a method for the preparation of taxane derivatives having the formula (I) and pharmaceutical compositions which contain the derivatives thus obtained. In formula (I), R is hydrogen or acetyl, R.sub.1 is benzoyl or R.sub.2 --O--CO wherein R.sub.2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl and Het is a 5-membered optionally substituted aromatic heterocycle (thiophene, tiazole, furan, pyrrole, imidazole, oxazole, isoxazole, pyrazole). The products of formula (I) have remarkable antitumor and antileukemia properties.

Abstract: This invention relates to novel anhydrides of general formula (I), ##STR1## wherein Ar is an aryl radical, and either R.sub.1 is C.sub.6 H.sub.5 --CO or (CH.sub.3).sub.3 C--O--CO, R.sub.2 is a hydrogen atom and R.sub.3 is a hydroxy function protective grouping, or R.sub.1 is (CH.sub.3).sub.3 C--O--CO and R.sub.2 together form a saturated 5 or 6-membered heterocyclic ring; preparation thereof; and uses thereof for preparing taxane derivatives having general formula (III), ##STR2## wherein R=H, acetyl; R.sub.1 is C.sub.6 --H.sub.5 --CO or (CH.sub.3).sub.3 C--O--CO), and having antitumoral properties.

Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is free or esterified carboxy, hydroxymethyl or formyl,R.sub.2 and R.sub.4 are each independently of the other aliphatic, cycloaliphatic-aliphatic, araliphatic or heteroarylaliphatic radicals andR.sub.3 is azido, or amino that is aliphatically or araliphatically substituted and/or protected by an amino-protecting group,and the salts thereof, are valuable intermediates in the preparation of medicinal active ingredients, for example of compounds of formula II ##STR2## wherein R.sub.A is an aromatic or heteroaromatic radical,R.sub.2 and R.sub.4 are each independently of the other aliphatic, cycloaliphatic, cycloaliphaticaliphatic or araliphatic radicals,R.sub.3 is unsubstituted or N-mono- or N,N-di-lower alkylated or N-lower alkanoylated amino, andR.sub.B is an aliphatically, cycloaliphatically or heteroaromatically-aliphatically substituted amino group,and the salts thereof, which can be used, for example, as antihypertensives.

Abstract: Novel water soluble carbodiimides, and intermediates or derivatives thereof, such as isoureas or isothioureas, are described. A particularly preferred embodiment is bis[4-(2,2-dimethyl-1,3-dioxolyl)methyl] carbodiimide (BDDC), which can be synthesized efficiently from 1,2-isopropylideneglycerol (solketal). The isoureas are effective esterifying agents. The corresponding N-protected amino acid tert-butyl, benzyl, isopropyl, ethyl, and methyl esters can be synthesized in high yield under neutral conditions, with no urea residue after simply washing with aqueous acid. Amino acid couplings utilizing carbodiimide embodiments give peptides in good yield, free of carbodiimide by-products, after washing with dilute acid, while racemization-free peptides are also obtained.

Abstract: A process for producing intermediate compounds 2-deoxy 2,2-difluoro-.beta.-D-ribo-pentopyranose (III) from 3,3-difluoro-4,5,6-O-trihydroxy-5,6-O-(1-ethylpropylidene)hexene (I). The process of preparing intermediate compound (I) involves reacting D-glyceraldehyde pentanide with an organometallic complex of 3-bromo-3,3-difluoropropene. The process of preparing intermediate compound (III) involves ozonolysis and then hydrolysis. The intermediate compounds (I) and (III) are used in the preparation of 2'-deoxy-2',2'-difluorocytidine which is an antiviral agent.