Abstract: The present invention concerns novel paclitaxel derivatives, their use as antitumor agents, and pharmaceutical formulations.

Abstract: This invention relates to a retinoid mpound of formula I ##STR1## in which Y is --CO--NH--, --CR.sup.2 .dbd.CR.sup.3 --, --CO--O--, --O--CO--, --C(.dbd.S)--NH--, --C.tbd.C--, --O--CH.sub.2 --, --CH.sub.2 --O--, or --CH.sub.2 --CH.sub.2 --;A is --(CH.sub.2).sub.t -- or a bond;Q is phenyl optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen, or --CO.sub.2 R.sup.4 ;R.sup.1 is --CO.sub.2 Z, --CONHR.sup.5, C.sub.1-6 alkyl, --CH.sub.2 OH, or --CHO;R.sup.2, R.sup.3, R.sup.4, R.sup.5, and Z are independently hydrogen or C.sub.1-6 alkyl;t is one to six.

Abstract: The present invention concerns water-soluble amino acid derivatives of paclitaxel, their use as antitumor agents, and pharmaceutical compositions containg the compounds.

Abstract: R.sup.g is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or a radical of the formula --W--R.sup.x in which W is a bond, C.sub.2-6 alkenediyl, or --(CH.sub.2).sub.t --, in which t is one to six; and R.sup.x is naphthyl, phenyl, or heteroaryl, and furthermore R.sup.x can be optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups;R.sup.2 is --OCOR, H, OH, --OR, --OSO.sub.2 R, --OCONR.sup.o R, --OCONHR, --OCOO(CH.sub.2).sub.t R, or --OCOOR; andR and R.sup.o are independently C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl, C.sub.2-6 alkynyl, or phenyl, optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups.Further provided by this invention are pharmaceutical formulations and intermediates for the the preparation of deoxy taxols of formula I. A method of treating mammalian tumors using a compound of formula I is also provided.

Abstract: The present invention provides paclitaxel derivatives of formula I ##STR1## in which R.sup.1 is --COR.sup.z, in which R.sup.z is RR.sup.o N--, RHN--, RO-- or R;R.sup.2 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or a radical of the formula --W--R.sup.x in which W is a bond, C.sub.2-6 alkenediyl, or --(CH.sub.2).sub.t --, in which t is one to six; and R.sup.x is naphthyl, phenyl, or heteroaryl, and furthermore R.sup.x can be optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups;R and R.sup.o are independently C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl, C.sub.2-6 alkynyl, or phenyl, optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups.Also provided by this invention are pharmaceutical formulations (compositions) and a method of treating mammalian tumors with a compound of formula I.

Abstract: The present invention provides paclitaxel derivatives of formula I ##STR1## in which R.sup.1 is --COR.sup.z in which R.sup.Z is RO-- or R;R.sup.2 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or a radical of the formula --W--R.sup.x in which W is a bond, C.sub.2-6 alkenediyl, or --(CH.sub.2).sub.t --, in which t is one to six; and R.sup.x is naphthyl, phenyl, or heteroaryl, and furthermore R.sup.x can be optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups;R.sup.a is --OCOR, H, OH, --OR, --OSO.sub.2 R, --OCONR.sup.o R, --OCONHR, --OCOO(CH.sub.2).sub.t R, or --OCOOR;R.sup.b and R.sup.c are both hydroxy or together form a bond with the carbon atoms to which they are attached; andR and R.sup.o are independently C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl, C.sub.2-6 alkynyl, or phenyl, optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.

Abstract: The present invention relates to new 3-guanidinoalkyl-2-azetidinones of the formula ##STR1## wherein: U and W can be the same or different and are selected from the group consisting of hydrogen and an amino protecting group;n is 1 to 3;X is a member selected from the group consisting of hydrogen, trialkylsilyl, arylsulfonyl, amino substituted arylsulfonyl, alkylsulfonyl, arylaminocarbonyl, alkylcarbonyl and arylcarbonyl; andY is a member selected from the group consisting of hydrogen, arylalkenyl, arylalkyl, formyl, carboxy, alkoxycarbonyl, acyloxy, arylthio, arylsulfinyl, arylsulfonyl, alkylthio, alkylsulfinyl, alkylsulfonyl, arylaminocarbonyl, the radical ##STR2## in which R is hydrogen, alkyl or arylalkyl, and the radical ##STR3## in which m is 1 to 3 and R' is hydrogen or --CO.sub.2 R" wherein R" is hydrogen, alkyl or arylalkyl.The novel azetidinones of the present invention exhibit anti-thrombin and anti-trypsin activities and are thus useful in controlling blood coagulation and treating pancreatitis.

Abstract: Thymidine kinase inhibitor of formula I ##STR1## in which R is C.sub.1-6 alkyl or AR(CH.sub.2).sub.n --, wherein Ar represents phenyl optionally substituted with one to five same or different halogen, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; and n equals one to six.A further aspect of the present invention provides a method of inhibiting viral thymidine kinase. Yet another aspect of the invention relates to treating herpes simplex viral infections in mammals. Yet another aspect of the invention provides a pharmaceutical formulation.

Abstract: The present invention relates to a process for the preparation of (3R, 4S)-3-hydroxy-4-phenyl-2-azetidinone derivatives which are useful intermediates in the synthesis of taxol from baccatin III, said process comprises reacting an acyloxyacetyl halide with an imine derived from L-threonine; and to compounds of formula (III) which are produced in said process: ##STR1## wherein Ar is phenyl; R.sup.1 is hydrogen, an acyl radical of a carboxylic acid, or a carbonic acid ester radical; R.sup.2 is hydrogen or a carboxy protecting group; and R.sup.3 is hydrogen or a hydroxy protecting group.

Abstract: This invention relates to a fluorinated taxol of formula I ##STR1## in which R.sup.1 is --COR.sup.z in which R.sup.z is RO-- or R;R.sup.g is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or a radical of the formula --W--R.sup.x in which W is a bond, C.sub.2-6 alkenediyl, or --(CH.sub.2).sub.t --, in which t is one to six; and R.sup.x is naphthyl, furyl, thienyl or phenyl, and furthermore R.sup.x can be optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups;R.sup.2 is --OCOR, H, OH, --OR, --OSO.sub.2 R, --OCONR.sup.o R, --OCONHR, --OCOO(CH.sub.2).sub.t R, or --OCOOR; andR and R.sup.o are independently C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl, C.sub.2-6 alkynyl, or phenyl, optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups.

Abstract: The present invention is directed to novel taxol derivatives useful as anti-tumor agents. Also provided by this invention is pharmaceutical formulations and methods of treating mammalian tumors with the compounds of this invention.

Abstract: This invention relates to a novel process for making a cephem of formula II from a 2-(3-amino-2-oxo-azetidin-1-yl)-2,3-butadienoate intermediate of formula I using an organo-copper reagent. In another aspect, this invention is concerned with said intermediate. ##STR1## In the compounds of Scheme (A), R.sup.1 is a conventional amino protecting group or an acyl group; R.sup.2 is an aromatic heterocyclic or aryl group; R.sup.3 is a conventional carboxy protecting group or --CO.sub.2 R.sup.3 taken together forms a physiologically hydrolyzable ester; and R.sup.4 is a group selected from the group consisting of C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, cyclic C.sub.3-6 alkyl, and aryl; and n is 0 or 2.

Abstract: The present invention provides BU-4641V of the formula: ##STR1## This invention also provides a biologically pure culture of BU-4641V producing Arthrinium sp. FA1744. Another aspect of the invention provides a process for preparing BU-4641V. Yet further aspect of the present invention provides a method for treating mammalian tumors and bacterial or viral infections.

Abstract: An antitumor compound of formula I ##STR1## in which R.sup.1 is --COR.sup.z in which R.sup.z is t-butyloxy, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or phenyl, optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups;R.sup.2 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or a radical of the formula --W--R.sup.x in which W is a bond, C.sub.2-6 alkenediyl, or --(CH.sub.2).sub.t --, in which t is one to six; and R.sup.x is naphthyl, furyl, thienyl or phenyl, and furthermore R.sup.x can be optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups;R.sup.3 is OCOR, --OCOOR, H, or OH; R.sup.4 is hydrogen; or R.sup.3 and R.sup.4 jointly form a carbonyl group; and R is C.sub.1-6 alkyl.

Abstract: The present invention relates to new 3-guanidinoalkyl-2-azetidinones of the formula ##STR1## wherein: U and W can be the same or different and are selected from the group consisting of hydrogen and an amino protecting group;n is 1 to 3;X is a member selected from the group consisting of hydrogen, trialkylsilyl, arylsulfonyl, amino substituted arylsulfonyl, alkylsulfonyl, arylaminocarbonyl, alkylcarbonyl and arylcarbonyl; andY is a member selected from the group consisting of hydrogen, arylalkenyl, arylalkyl, formyl, carboxy, alkoxycarbonyl, acyloxy, arylthio, arylsulfinyl, arylsulfonyl, alkylthio, alkylsulfinyl, alkylsulfonyl, arylaminocarbonyl, the radical ##STR2## in which R is hydrogen, alkyl or arylalkyl, and the radical ##STR3## in which m is 1 to 3 and R' is hydrogen or --CO.sub.2 R" wherein R" is hydrogen, alkyl or arylalkyl.The novel azetidinones of the present invention exhibit anti-thrombin and anti-trypsin activities and are thus useful in controlling blood coagulation and treating pancreatitis.

Abstract: The present invention relates to new cephalosporins of the formula ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or carboxy, with the proviso that both cannot be the same;R.sup.3 is hydrogen or acetyl; andR.sup.4 is a radical selected from the group consisting of ##STR2## in which n is 1 or 2, R.sup.5 is hydrogen or acetyl, and R.sup.6 is hydrogen, a lower C.sub.1-3 alkyl, or a radical selected from the group consisting of ##STR3## in which n and R.sup.5 are as defined above. In another aspect, this invention relates to processes for the preparation of the compounds of Formula I, to pharmaceutical compositions containing at least one compound of Formula I, and to intermediates in their preparation.

Abstract: A compound of formula I ##STR1## wherein X is sulfur or CH.sub.2 ;R.sup.1 is hydrogen, hydroxy, amino, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, phenyl optionally substituted with one to three C.sub.1-6 alkyl, C.sub.1-6 alkyloxy or hydroxy, C.sub.1-6 alkylthio, phenylthio optionally substituted with one to three C.sub.1-6 alkyl or C.sub.1-6 alkyloxy on the phenyl ring, phenylmethyloxy optionally substituted with one to three C.sub.1-6 alkyl or C.sub.1-6 alkyloxy on the phenyl ring, 1-morpholino, C.sub.1-6 alkyloxy, C.sub.2-6 alkenylmethyloxy, C.sub.3-6 alkynylmethyloxy, C.sub.1-6 alkylamino, C.sub.1-6 dialkylamino or a radical selected from the group consisting of ##STR2## in which n is 0 to 3, R.sup.5 is C.sub.1-6 alkyl or hydrogen, and R.sup.3 and R.sup.4 are independently C.sub.1-6 alkyl;R.sup.2 is hydrogen, a conventional amino protecting group or an acyl group;R.sup.0 is hydrogen or a conventional carboxy protecting group, or --CO.sub.2 R.sup.

Abstract: This invention relates to novel antibiotic cephalosporin derivatives of the formula ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, or a radical of the formula ##STR2## in which R.sup.3 and R.sup.4 are independently hydrogen, methyl or ethyl, or R.sup.3 and R.sup.4, taken together with the carbon atom to which they are attached, may be a cycloalkylidene ring containing from 3 to 6 carbon atoms;R.sup.2 is a radical selected from the group consisting of ##STR3## wherein R.sup.5 is hydrogen or C.sub.1-6 alkyl. This invention further relates to compounds of formula I and their pharmaceutically acceptable salts, physiologically hydrolyzable esters or solvates.

Abstract: This invention relates to a fluorinated taxol of formula I ##STR1## in which R.sup.1 is benzoyl or t-butyloxycarbonyl; R.sup.2 is acetoxy, hydrogen or hydroxy; and the wavy line indicates either the .alpha.- or the .beta.-configuration.Further provided by this invention are pharmaceutical formulations and useful intermediates for the fluorinated taxols of formula I. A method of treating mammalian tumors using a compound of formula I is also provided.

Abstract: This invention relates to a compound of formula I ##STR1## or a pharmaceutically acceptable salt thereof, in which R.sup.2 is a radical of the formula ##STR2## in which R.sup.a and R.sup.b are independently hydrogen or C.sub.1-6 alkyl, said C.sub.1-6 alkyl being optionally substituted with hydroxy, phosphono, phosphonooxy, carboxy or di(C.sub.1-6 alkyl) amino; or NR.sup.a R.sup.b together represents a radical of the formula ##STR3## in which y is one to three, and R.sup.a is as defined above; R.sup.p and R.sup.r are independently same or different C.sub.1-6 alkyl;R.sup.1 is hydrogen or a radical Z of the formula ##STR4## in which Q is --(CH.sub.2).sub.f --, optionally substituted with one to six same or different C.sub.1-6 alkyl or C.sub.3-6 cycloalkyl, or a carbon atom of said --(CH.sub.2).sub.f -- radical may also be a part of C.sub.3-6 cycloalkylidene;R.sup.3 and R.sup.4 are independently hydrogen or C.sub.1-6 alkyl, or R.sup.3 and R.sup.