Abstract: The present invention relates to 12,13-position modified epothilone derivatives, methods of preparation of the derivatives, and intermediates therefor.

Abstract: Novel non-steroidal compounds are provided which are glucocorticoid receptor modulators which are useful in treating diseases requiring glucocorticoid receptor agonist or antagonist therapy such as obesity, diabetes, inflammatory and immune disorders, and have the structure 1

Abstract: The present invention relates to compounds useful in the treatment of cancer or other proliferative diseases represented by formula I: wherein: Q is selected from the group consisting of M is O, NR9, or CR10R11; X is O or NH; and the R groups are as defined, and therapeutic compositions containing them alone or in combination with other therapeutic agents useful in the treatment of cancer or other proliferative diseases.

Abstract: Compound having the formula (I), 1

Abstract: The present invention relates to a process for the preparation of intermediates useful in the synthesis of epothilone analogs by initially enzymatically degrading certain epothilone compounds to form ring-open structures containing a carboxyl group which is esterified, the hydroxyl groups on the moiety protected and the resulting compound oxidized by, e.g. ozone, to form a first intermediate. The first intermediate can be reacted with a triphenylphosphine adduct to yield a compound containing an ester group at position 1 which is subsequently hydrolyzed to form a second intermediate.

Abstract: The present invention relates to compounds of the formula 1

Abstract: The present invention relates to compounds useful in the treatment of cancer or other proliferative diseases represented by formula I: 1

Abstract: The present invention relates to epothilone derivatives, having the following formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1-R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.

Abstract: Disclosed are quinoline and benzazepine derivatives that inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogenic protein Ras. Thus, the compounds are useful as anti-cancer agents. The compounds are also useful in the treatment of diseases other than cancer.

Abstract: The present invention relates to a process for the preparation of intermediates useful in the synthesis of epothilone analogs by initially enzymatically degrading certain epothilone compounds to form ring-open structures containing a carboxyl group which is esterified, the hydroxyl groups on the moiety protected and the resulting compound oxidized by, e.g. ozone, to form a first intermediate. The first intermediate can be reacted with a triphenylphosphine adduct to yield a compound containing an ester group at position 1 which is subsequently hydrolyzed to form a second intermediate.

Abstract: The present invention relates to 12,13-position modified epothilone derivatives, methods of preparation of the derivatives, and intermediates therefor.

Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras ocogene expression, is effected by compounds of the formulas their enantiomers, diastereomers, and pharmaceutically acceptable salts, prodrugs and solvates thereof inhibit farnesyl protein transferase which is an enzyme involved in ras oncogene expression.

Abstract: The present invention relates to 12,13-position modified epothilone derivatives, methods of preparation of the derivatives and intermediates therefor.

Abstract: Disclosed are quinoline and benzazepine derivatives that inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogenic protein Ras. Thus, the compounds are useful as anti-cancer agents. The compounds are also useful in the treatment of diseases other than cancer.

Abstract: The present invention relates to 12,13-position modified epothilone derivatives, methods of preparation of the derivatives and intermediates therefor.

Abstract: The present invention relates to a process for the preparation of intermediates useful in the synthesis of epothilone analogs by initially enzymatically degrading certain epothilone compounds to form ring-open structures containing a carboxyl group which is esterified, the hydroxyl groups on the moiety protected and the resulting compound oxidized by, e.g. ozone, to form a first intermediate. The first intermediate can be reacted with a triphenylphosphine adduct to yield a compound containing an ester group at position 1 which is subsequently hydrolyzed to form a second intermediate.

Abstract: The present invention relates to a process to produce ring opened epothilones and the novel ring opened epothilones produced thereform.

Abstract: The invention as claimed is directed to a process for making an epothilone having the following structures from ones having an oxiranyl moiety, by reacting a compound having the latter structure with a metal or metal-assisted reagent. Said metal or metal-assisted reagent is selected from the group consisting of a) reactive metallocenes; b) [N2C(CO2Me)2, cat Rh2,(OAC)4]; c) [N2C(CO2Me)2, cat[(n-C7H15CO2)2 Rh]2]; d) [Zn—Cu, EtOH]; e) [Mg(Hg), MgBr]; f) Cr; g) [FeCl3, n-BuLi]; h) [TiCl3, LiAlH4]; i) [TiCl4, Zn]; j) [WCl6, LiAlH4,]; k) [NbCl5, NaAlH4]; l) [VCl3,Zn] and m) [WCl6, n-BuLi].

Abstract: The present invention relates to a stereospecific process to produce aziridinyl epothilones from oxiranyl epothilones and the intermediates derived therein.

Abstract: The present invention relates to a stereospecific process to produce aziridinyl epothilones from oxiranyl epothilones and the intermediates derived therein.