Abstract: Taxol dosages of about 135 mg/m2 or greater are administered via infusions of less than 6 hours duration; the method makes it possible to provide taxol infusions on an out-patient basis to patients who do not otherwise require hospitalization. In a preferred embodiment, about 135 mg/m2 of taxol in a cremaphor emulsion is infused over a 3 hour duration, following patient pretreatment with steroids, antihistamines, and H2-receptor antagonists sufficient to prevent fatal anaphylactic-like reactions, and preferably sufficient to reduce the occurrence of severe anaphylactic-like reactions in greater than 90% of patients treated. In an alternative embodiment, between 135 mg/m2 and about 175 mg/m2 of taxol is provided in a 3-hour infusion, following pretreatment to minimize hypersensitivity responses. A method for rechallenging patients with taxol after episodes of acute hypersensitivity reactions is also disclosed, thus enabling patients to continue taxol therapy who would otherwise be deprived of treatment.

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: Process for synthesizing paclitaxel by treating baccatin III with a strong base in a solvent, adding an electrophile to the solution to form a 7-O-protected baccatin III derivative, reacting the 7-O-protected baccatin III derivative with a protected paclitaxel sidechain in a solvent such that the protected paclitaxel sidechain is coupled to the 13-hydroxyl of the 7-O-protected baccatin III, and subsequently deprotecting the protected paclitaxel sidechain and the 7-O protecting group to form paclitaxel, and intermediates used therein.

Abstract: A process for the synthesis of a C-4 methyl carbonate paclitaxel analog from 10-deacetylbaccatin III by the selective reduction of the acetate at the C-4 position of 10-deacetylbaccatin using Red-Al.

Abstract: A process for the synthesis of paclitaxel from 10-deacetylbaccatin-III which is protected at the 7-position with a dialkylalkoxysilyl protecting group having the formula —Si(R)2(OR′).

Abstract: A ras-farnesyltransferase inhibitor complex formed of ras-farnesyltransferase inhibitor or a pharmaceutically acceptable salt thereof, of the formula I wherein n is 0 or 1; R1 is selected from Cl, Br, phenyl, pyridyl or cyano; R2 is aralkyl; R3 is selected from lower alkyl, aryl or substituted aryl or heterocyclo; Z1 is selected from CO, SO2, CO2, or SO2NR5, R5 is selected from hydrogen, lower alkyl or substituted alkyl; and sulfobutylether-7-&bgr;-cyclodextrin or 2-hydroxypropyl-&bgr;-cyclodextrin is provided. The complex has unexpectedly high aqueous solubility of the ras-farnesyltransferase inhibitor and is useful for its intravenous delivery to humans with cancer. Also provided is a method for forming the complex. The ras-farnesyltransferase inhibitors are useful as anti-tumor agents.

Abstract: The present invention describes compounds of formula I and enantiomers, diastereomers and pharmaceutically acceptable salts thereof. The formula I compounds are protein kinase inhibitors and are useful in the treatment of proliferative diseases, for example, cancer, inflammation and arthritis. They may also be useful in the treatment of Alzheimer's disease, chemotherapy-induced alopecia, and cardiovascular disease.

Abstract: Novel reaction conditions for the cleavage of silyl ethers from silyl protected taxane precursors to afford paclitaxel and paclitaxel analogues in high yield and quality are described. Paclitaxel is prepared from a taxane precursor by treating the taxane precursor with a strong acid such as trifluoroacetic acid in a solvent such as aqueous acetic acid, such that the amount and number of side reactions and taxane impurities are significantly minimized. Also desribed are the crystallization methods for the isolation of paclitaxel in either of the two crystal forms A or B. Paclitaxel and paclitaxel analogues are anti-cancer agents.

Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formula ##STR1## and their enantiomers, diastereomers, and their pharmaceutically acceptable salts, including prodrugs and solvates thereof.The compounds of formula I are useful in the treatment of a variety of cancers. In addition, the formula I compounds may also be useful in the treatment of diseases other than cancer.

Abstract: The novel compounds of formula I: ##STR1## (R.sup.1, R.sup.2 and Hal are defined in the specification) show selective fungicidal activity. The new compounds are processed with carriers and adjuvants to fungicidal compositions.

Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof for use as inhibitors of cyclin dependent kinases, wherein:X is O, S(O).sub.m ;Y is alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl;R.sub.1 is hydrogen or lower alkyl;R.sub.2 is alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, --O-alkyl, --O-aryl, --NR.sub.4 R.sub.5 ;R.sub.3 is hydrogen or lower alkyl;R.sub.4 is hydrogen, alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, --O-alkyl, --O-aryl;R.sub.5 is hydrogen, alkyl, aryl, alkylaryl, heteroaryl, alkylheteroaryl, cycloalkyl, alkylcycloalkyl, heterocycloalkyl, alkylheterocycloalkyl, --O-alkyl, --O-aryl; andm is 0, 1 or 2.

Abstract: A novel process for the production of tertiary amines by reductive alkylation of second amine using hydrosilane and a Lewis acid is disclosed. The novel process has applications in the preparation of imidazole-containing benzodiazepines, inhibitors of farnesyl protein transferase.

Abstract: The present invention provides a composition for attracting termites containing a steroid derivative of formula I ##STR1## The present invention also provides a method for attracting or controlling termites with the composition.

Abstract: An effective and efficient process for the preparation of chloro-benzoylchlorides of formula I, ##STR1## (n is defined in the specification). In this process a a chloro-trichloromethylbenzene of formula II ##STR2## is treated with water acid in the presence of a Lewis at temperatures below 80.degree. C. The compounds obtained according to this process can be used to prepare certain chloro-substituted benzophenones.

Abstract: New herbicidal pyridine and pyrimidine derivatives of general formula (I), ##STR1## wherein Z represents a nitrogen atom or a C--H group; A represents an optionally substituted aryl group or an optionally substituted 5- or 6-membered nitrogen-containing heteroaromatic group; n represents an integer from 0 to 2 and R.sup.1 or each R.sup.1 independently represents a hydrogen atom or an optionally substituted alkyl, alkoxy, alkylthio or dialkylamino group; m represents an integer from 0 to 5 and R.sup.2 or each R.sup.2 independently represents a hydrogen or a halogen atom or an optionally substituted alkyl, haloalkyl, haloalkoxy, alkoxy, alkylthio group or a nitro, cyano or a halosulphonyl group; and X represents an oxygen or sulphur atom.

Abstract: The present invention provides pH-sensitive microcapsules, compositions containing them, methods for their preparation and methods for their use.

Abstract: The novel compounds of formula I: whereinR.sup.1 represents an optionally substituted alkyl, alkenyl, alkynyl, alkadienyl, or aryl group, or an optionally substituted cycloalkyl or cycloalkenyl group, in which one CH.sub.2 group may also be replaced by O, S or NR.sup.2, in which R.sup.2 represents a hydrogen atom or an alkyl group;X represents a hydrogen or halogen atom, or an alkoxy, aryloxy, aralkyloxy, haloalkoxy, alkylthio, cyano, amino, alkylamino or dialkylamino group;L.sup.1, L.sup.2, L.sup.3, L.sup.4 and L.sup.5 each independently represent an hydrogen or halogen atom or an optionally substituted alkyl or alkoxy group or a nitro or cyano group show selective fungicidal activity. The new compounds are processed with carriers and, optionally, adjuvants, to afford fungicidal compositions, useful in agricultural applications.

Abstract: Herbicidal 2-(hetero)aryloxy-6-arylpyridines and 2-Aryl-4-(hetero)aryloxypyrimidinesNew herbicidal pyridine and pyrimidine derivatives of general formula (1), ##STR1## wherein Z represents a nitrogen atom or a C--H group; A represents an optionally substituted aryl group or an optionally substituted 5- or 6-membered nitrogen-containing heteroaromatic group; n represents an integer from 0 to 2 and R.sup.1 or each R.sup.1 independently represents a hydrogen atom or an optionally substituted alkyl, alkoxy, alkylthio or dialkylamino group; m represents an integer from 0 to 5 and R.sup.1 or each R.sup.1 independently represents a hydrogen or a halogen atom or an optionally substituted alkyl, haloalkyl, haloalkoxy, alkoxy, alkylthio group or a nitro, cyano or a halosulphonyl group; and X represents an oxygen or sulphur atom.

Abstract: The novel compounds of formula I: ##STR1## (A, L, n and R.sup.1 through R.sup.4 are defined in the specification) show selective fungicidal activity. The new compounds can be combined with carriers and adjuvants to form fungicidal compositions.

Abstract: The novel compounds of formula I: ##STR1## (R.sup.1, R.sup.2, R.sup.3, L.sup.1, L.sup.2 and Hal are defined in the specification) show selective fungicidal activity. These compounds may be processed with carriers, and optionally an adjuvant, to produce fungicidal compositions.