Abstract: Taxol (I) is a complex deterpene which is currently considered the most exciting lead in cancer chemotherapy. Taxol possesses high cytotoxicity and strong antitumor activity against different cancers which have not been effectively treated by existing antitumor drugs. However, taxol has a problem with solubility in aqueous media, which may impose some serious limitation in its use. Taxotére (III) seems to have antitumor activity superior to taxol with better bioavailability. Taxotére has a modified taxol structure with a modified C-13 side chain. This fact strongly indicates that modification on the C-13 side chain would provide a new series of taxol and Taxotére analogues which may have higher potency, better bioavailability and less unwanted toxicity. The present invention provides efficient and practical methods for the syntheses of Taxotére and its analogues through &bgr;-lactam intermediates and their coupling with baccatin III.

Abstract: A process for the preparation of a taxane derivative of the formula in which R2 represents an RO—, RS— or RR′N— in which R represents an unsubstituted or substituted straight chain or branched alkyl, alkenyl or alkynyl, or cycloalkyl, saturated heterocyclic, cycloalkenyl, unsaturated heterocyclic, aryl or heterocyclic aromatic; R′ is a hydrogen or R defined above; R and R′ can be connected to form together with the nitrogen a cyclic structure; Y is oxygen or sulfur; R3 represents an unsubstituted or substituted straight chain or branched alkyl, alkenyl or alkynyl radical, an unsubstituted or substituted cycloalkyl, cycloalkenyl or an unsubstituted or substituted aryl; which comprises reacting a &bgr;-lactam of the formula in which R311 represents a radical R3 defined above or a protected R3 whenever R3 includes one or more active hydrogens; with a baccatin III derivative of the formula: in which M is an alkali metal

Abstract: This invention relates to a taxoid of the formula (I): ##STR1## wherein R.sup.1 is a C.sub.3 -C.sub.5 alkyl or alkenyl or trifluoromethyl radical;R.sup.2 is a C.sub.3 -C.sub.5 branched alkyl radical;R.sup.3 and R.sup.4 are independently selected from hydrogen and hydroxyl protecting groups including functional groups which increase the water solubility of the taxoid antitumor agent;R.sup.5 is a hydrogen, an acyl radical, or an alkoxylcarbonyl or carbamoyl radical; andR.sup.6 is an acyl radical.The compounds of formula I are useful as antitumor agents or their precursors. This invention also relates to a pharmaceutical composition having antineoplastic activity comprising the compound of formula (I) and a physiologically acceptable carrier and method of treatment using the compound of formula I.

Abstract: This invention relates to a taxoid of the formula (I) ##STR1## wherein R.sup.1 is 1-propenyl radical;R.sup.2 is a C.sub.3 -C.sub.5 branched alkyl radical;R.sup.3 and R.sup.4 are independently selected from hydrogen and hydroxyl protecting groups including functional groups which increase the water solubility of the taxoid antitumor agent;R.sup.5 represents a hydrogen or a hydroxyl protecting group;R.sup.6 represents an acyl radical,which are useful as antitumor agents or their precursors. A pharmaceutical composition having antineoplastic activity comprising the compound of formula (I) and a physiologically acceptable carrier and method of treatment are also disclosed.

Abstract: A process comprising subjecting at least one compound containing at least one carbon--carbon double bond or at least one carbon--carbon triple bond, hydrogen and carbon monoxide, to a hydrocarbonylation reaction in supercritical carbon dioxide, in the presence of a Group VIII transition metal catalyst precursor, and a phosphite ligand.

Abstract: The present invention is directed to novel taxoids possessing strong reversing activities for drug-resistance associated with anti-cancer agents, the preparation of these reversal agents and pharmaceutical compositions thereof. The new taxoids of the present invention have the formula (I).

Abstract: The present invention is directed to novel taxanes useful as chemotherapeutic agents or their precursors. Processes for preparing the novel taxanes include coupling reactions, in the presence of a base, of baccatin of formula (III) or (IV) ##STR1## with .beta.-lactams of formula (V). ##STR2## The invention also provides pharmaceutical compositions including the novel taxanes and methods for treatment of certain cancers with these new compounds.

Abstract: The present invention is directed to novel taxanes useful as chemotherapeutic agents or their precursors. Processes for preparing the novel taxanes include coupling reactions, in the presence of a base, of baccatin of formula (III) or (IV) ##STR1## with .beta.-lactams of formula (V). ##STR2## The invention also provides pharmaceutical compositions including the novel taxanes and methods for treatment of certain cancers with these new compounds.

Abstract: The present invention is directed to novel taxanes useful as chemotherapeutic agents or their precursors. Processes for preparing the novel taxanes include coupling reactions, in the presence of a base, of baccatin of formula (III) or (IV) ##STR1## with .beta.-lactams of formula (V). ##STR2## The invention also provides pharmaceutical compositions including the novel taxanes and method for treatment of certain cancers with these new compounds.

Abstract: The present invention provides synthetic antiaggregatory agents for preventing inhibition of fibrinogen-platelet binding. These anti-aggregatory agents have the general formulas (1)-(5).H--[--(AA.sub.i).sub.i --R--G--D--(AA.sub.j).sub.j --].sub.n --Cx (1)[Ri--C(O)--R--G--D--(AA.sub.j).sub.j --].sub.n --CX (2)Cy--[--AA.sub.i).sub.i --R--G--D--(AA.sub.j).sub.i --].sub.n --Z (3)H--[--(AA.sub.i).sub.i --R--G--D--(AA.sub.j).sub.j --].sub.n --CZ--[--(AA.sub.k).sub.k --R--G--D--(AA.sub.l).sub.l --].sub.m --Z (4)[R.sub.1 --C(O)--R--G--D--(AA.sub.i).sub.i --].sub.n --CZ[--(AA.sub.j).sub.j ]--R--G--D--(AA.sub.k).sub.k --].sub.m --Z (5)in which: R=Arg; G=Gly; D=Asp; AA.sub.i, AA.sub.j, AA.sub.k and AA.sub.l = alpha-, beta- and omega-amino acid residues; (AA.sub.i).sub.i (AA.sub.j).sub.j =peptide chains having the same or different amino acid residues; (AA.sub.k).sub.k =peptide chains having the same or different amino acid residues; (AA.sub.l).sub.

Abstract: The reaction between a hydroxyacetic acid derivative bearing an oxygen protecting group and a chiral auxiliary group and an imine produces chiral .beta.-lactams. Hydrolysis of the chiral .beta.-lactams produces chiral amino acid analogs.

Abstract: The present invention relates to analgesic enkephalin derivatives represented by the following formula:Tyr-A.sub.1 -A.sub.2 -A.sub.3 -A.sub.4 SEQ ID NO:5 (1)and the acid salts thereof, wherein Tyr is L-tyrosine, A.sub.1 or A.sub.2 is a glycine, and that which is not a glycine is an optically active trifluoro amino acid of the formula: ##STR1## wherein n is an integer from 1-3 and m is 1 or 2; A.sub.3 is L-Phenylalanine, or N-methyl-(L)-phenylalanine, and A.sub.4 is L-Methionine, L-Met-OH, L-Met-ol or L-Met-NH.sub.2.

Abstract: A process for preparing a perfluoroalkyl-substituted compound is disclosed. The process comprises reacting a halopolyfluoroalkane having 1 to 20 carbon atoms with a compound selected from the group consisting of (1) a substituted or unsubstituted ethylene, (2) a substituted or unsubstituted acetylene and (3) a substituted or unsubstituted allylsilane, in the presence of a metal-carbonyl complex of the metal of the Group VIII of the Periodic Table. Alternatively, the reaction between the halopolyfluoroalkane and the substituted or unsubstituted allylsilane is effected under radical generating condition.

Abstract: A catalyst for isomerization consisting essentially of a salt or complex salt represented by the formula:[ML.sub.m ].sup.n+ [Y].sub.n.sup.- (I)where M is a metal of Group IB, IIA, IIB or VIII of the periodic table, L is a ligand, Y is a conjugated base of a Bronsted acid, m is 0, 1, 2, 3 or 4 and n is 1, 2 or 3.

Abstract: An .alpha.-trifluoromethylacrylate, which does not undergo radical homopolymerization, is easily and efficiently copolymerized with styrene or its derivatives by using a common radical polymerization initiator. The composition of the resultant copolymer does not greatly vary with the proportions of the monomers subjected to copolymerization and usually is close to an alternating copolymer.

Abstract: A process for preparing a 5-perfluoroalkyl-dihydrouracil derivative of the general formula ##STR1## wherein R.sub.f represents a perfluoroalkyl group, each of R.sup.1 and R.sup.2 represents a hydrogen atom, or an alkyl, cycloalkyl, aryl, aralkyl or heterocyclic group, and Y is an oxygen or sulfur atom, which comprises (a) reacting a compound of the general formula ##STR2## wherein X represents a halogen atom or hydroxyl group, with a urea derivative of the general formula ##STR3## provided that when X is a hydroxyl group and at least one of R.sup.1 and R.sup.2 is a hydrogen atom, said reaction is carried out in the presence of a condensing agent, or (b) cyclizing a compound of the general formula ##STR4## and a novel intermediate compound of the above formula (IV).

Abstract: A process of preparing 2-trifluoromethylpropanol by vapor phase contact reaction between 2-trifluoromethylpropanal trimer and hydrogen in the presence of a catalyst of which the principal component is reduced nickel. The hydrogenation reaction can easily be completed at about 30.degree.-150.degree. C. and at the atmospheric pressure. The starting material is hydrogenated nearly theoretically and with very high selectivity factor for 2-trifluoromethylpropanol.

Abstract: A process for the production of an N-acyl-.alpha.-amino acid represented by the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4, independently from each other, represent a hydrogen atom, an alkyl or cycloalkyl group which may be substituted, or an aryl or heteroaromatic group selected from the group consisting of furyl, pyrrolyl, pyridinyl, thienyl and indolyl which may be substituted, which comprises reacting an oxirane represented by the general formula ##STR2## wherein R.sup.1 and R.sup.2 are as defined above, an amide compound represented by the general formulaR.sup.3 CONHR.sup.4 (III)wherein R.sup.3 and R.sup.4 are as defined above, and carbon monoxide in the presence of hydrogen, a cobalt-containing catalyst, and a promoter composed of a compound containing a metal selected from Groups I, II, III and IV of the periodic table.

Abstract: A process for producing an aldehyde containing a perfluorocarbon group, which comprises hydroformylating an olefin containing a perfluorocarbon group represented by the general formula ##STR1## wherein R.sub.f represents a monovalent perfluorocarbon group, in the presence of a rhodium catalyst.

Abstract: There is provided a novel process for the preparation of a dipeptide represented by the formula: ##STR1## wherein Ar represents an aromatic group; R.sup.1 represents a hydrogen atom, an alkyl group or an aryl group; R.sup.2 represents a hydrogen atom, an alkyl group or an aromatic group; Y represents a hydroxy group, an amino group or an acylamino group, which comprises subjecting a .beta.-lactam compound represented by the formula: ##STR2## wherein Ar, R.sup.1 and R.sup.2 have the same meanings as defined above, and X represents a hydroxy group, an amino group or an acylamino group, an azido group or a benzyloxy group, to hydrogenolysis in the presence of a catalyst. The process can be practiced without any complicated procedure as seen in the conventional processes for the preparation of peptides.